Home Protein Tyrosine Kinase PDGFR inhibitor Sunitinib (SU11248) Malate

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Sunitinib (SU11248) Malate Tyrosine Kinase Inhibitor

Cat.No.S1042

Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Sunitinib (SU11248) Malate PDGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 532.56

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Quality Control

Batch: Purity: 99.60%
99.60

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 Kinase Assay Inhibition of PDGF-induced BrdU incorporation with IC50 of 0.007 μM 12646019
3T3 Growth Inhibition Assay Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation with IC50 of 0.01 μM 12646019
3T3 Function Assay Inhibition of Vascular endothelial growth factor receptor with IC50 of 0.05 μM 12646019
3T3 Kinase Assay 20 min DMSO Cellular inhibition of VEGF induced human KDR phosphorylation with IC50 of 0.022 μM 16162008
NIH3T3 Kinase Assay 20 min DMSO inhibit human KDR kinase expressed with IC50 of 0.018 μM 16162008
A549 Function Assay DMSO Inhibition of c-Met dependent HGF-induced human A549 cell migration with IC50 of 2 μM 18434145
DU145 Function Assay DMSO Inhibition of c-Met dependent HGF-induced human DU145 cell scattering with IC50 of 10 μM 18434145
KB3-1 Cytotoxic Assay 72 h DMSO Cytotoxicity against human P-gp-negative KB-3-1 cells with IC50 of 2.3 μM 19397322
KBV1 Cytotoxic Assay 72 h DMSO Cytotoxicity against human P-glycoprotein-expressing KBV1 cells with IC50 of 4.1 μM 19397322
A375 Cytotoxic Assay 72 h DMSO IC50=5.4 μM 19654408
RS4-11 Function Assay 2 h Inhibition of FLT3 autophosphorylation with IC50 of 0.0099 μM 19654408
RS4-11 Function Assay 2 h Inhibition of FLT3 ITD mutant autophosphorylation with IC50 of 0.034 μM 19654408
Sf9 Kinase Assay 30 min Inhibition of GST-tagged VEGFR expressed with IC50 of 0.185 μM 19854051
Ba/F3 Growth Inhibition Assay 72 h IC50=1.2 μM 20117004
BaPTC2 Growth Inhibition Assay 72 h IC50=0.22 μM 20117004
Sf9 Function Assay 1 h DMSO Inhibition of human recombinant His-tagged RET expressed with IC50 of 1.3 μM 20117004
H4 Cytotoxic Assay 10 μM Toxicity in human H4 cells 20350806
SF-539 Kinase Assay 333 μM 60 min DMSO Inhibition of PDGFRbeta phosphorylation with IC50 of 12.2 μM 20403700
U251 Kinase Assay 333 μM 60 min DMSO Inhibition of VEGFR2 phosphorylation with IC50 of 18.9 μM 20403700
A431 Kinase Assay Inhibition of PDGFRbeta expressed with IC50 of 12.2 μM 20558072
A431 Kinase Assay Inhibition of VEGFR2 expressed with IC50 of 18.9 μM 20558072
HepG2 Growth Inhibition Assay 72 h IC50=3.81 μM 20570526
Kasumi-1 Growth Inhibition Assay 72 h IC50=0.016 μM 20570526
RS4-11 Growth Inhibition Assay 72 h IC50=1 μM 20570526
THP1 Growth Inhibition Assay 72 h IC50=0.5 μM 20570526
Kasumi-1 Function Assay Inhibition of c-Kit autophosphorylation with IC50 of 0.015 μM 20833039
A549 Growth Inhibition Assay 16 h Antitumor activity against human A549 cells 21450463
HL60 Growth Inhibition Assay 16 h Antitumor activity against human HL60 cells 21450463
HUVEC Growth Inhibition Assay 16 h Inhibition of VEGF-induced cell proliferation with IC50 of 2.75 μM 21450463
HUVEC Growth Inhibition Assay 16 h Inhibition of bFGF-induced cell proliferation with IC50 of 4.04 μM 21450463
IM9 Growth Inhibition Assay 16 h Antitumor activity against human IM9 cells 21450463
K562 Growth Inhibition Assay 16 h Antitumor activity against human K562 cells 21450463
MDA-MB-231 Growth Inhibition Assay 16 h Antitumor activity against human MDA-MB-231 cells 21450463
H460 Cytotoxic Assay 72 h IC50=2.7 μM 21621880
SMMC7721 Cytotoxic Assay 72 h IC50=6.47 μM 21621880
WI38 Cytotoxic Assay 72 h IC50=8.56 μM 21621880
HEK293 Kinase Assay 100 nM 1 h does not inhibit VEGF-induced autophosphorylation of tyrosine 1175 residue on VEGFR2 expressed in HEK293 cells 21885287
HUVEC Function Assay 1 μM 24 h Antiangiogenic activity assessed as decrease in VEGF-induced cell migration 21963305
HUVEC Function Assay 1 μM 1 h Inhibition of ERK phosphorylation at Thr202/Tyr204 in VEGF-stimulated HUVEC 21963305
HUVEC Function Assay 1 μM 1 h Inhibition of eNOS phosphorylation at Ser-1172 in VEGF-stimulated HUVEC 21963305
HUVEC Kinase Assay 1 μM 1 h Inhibition of VEGFR2 phosphorylation at tyr-1175 in VEGF-stimulated HUVEC 21963305
HUVEC Function Assay 1 μM 1 h does not inhibit AKT phosphorylation at Ser-473 in VEGF-stimulated HUVEC 21963305
HL60 Cytotoxic Assay 50 μM 48 h DMSO IC50=15.5 μM 22019188
K562 Cytotoxic Assay 50 μM 48 h DMSO IC50=21.9 μM 22019188
PC3 Cytotoxic Assay 50 μM 48 h DMSO IC50=25.1 μM 22019188
SF-539 Kinase Assay 333 μM 60 min Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells with IC50 of 12.2 μM 22204741
HAEC Growth Inhibition Assay 100 μM 72 h Antiproliferative activity against human HAEC cells expressing VEGFR with IC50 of 0.1 μM 22444679
HT-29 Growth Inhibition Assay 100 μM 72 h Antiproliferative activity against human HT-29 cells expressing VEGFR with IC50 of 0.33 μM 22444679
MV4-11 Cytotoxic Assay 72 h IC50=0.003 μM 22452518
HepG2 Cytotoxic Assay 48 h IC50=13.24 μM 22483608
PC9 Cytotoxic Assay 48 h IC50=10.97 μM 22483608
CAKI-1 Growth Inhibition Assay 100 μM 48 h DMSO GI50=0.63 μM 22560627
EKVX Growth Inhibition Assay 100 μM 48 h DMSO GI50=7.9 μM 22560627
MCF7 Growth Inhibition Assay 100 μM 48 h DMSO GI51=2 μM 22560627
MDA-MB-435 Growth Inhibition Assay 100 μM 48 h DMSO GI52=2 μM 22560627
OVCAR3 Growth Inhibition Assay 100 μM 48 h DMSO GI53=3.2 μM 22560627
SNB19 Growth Inhibition Assay 100 μM 48 h DMSO GI54=10 μM 22560627
SW620 Growth Inhibition Assay 100 μM 48 h DMSO GI55=1.3 μM 22560627
TK10 Growth Inhibition Assay 100 μM 48 h DMSO GI56=6.3 μM 22560627
UACC257 Growth Inhibition Assay 100 μM 48 h DMSO GI57=4 μM 22560627
HAEC Cytotoxic Assay 100 μM 72 h DMSO Cytotoxicity against VEGFR expressing HAEC with IC50 of 0.1 μM 23131541
HT-29 Cytotoxic Assay 100 μM 72 h DMSO Cytotoxicity against VEGFR expressing human HT-29 cells with IC50 of 0.33 μM 23131541
HCT116 Function Assay 24 h DMSO Antimigratory activity assessed as inhibition of cell migration 23153200
HUVEC Function Assay 2 μM 18 h DMSO Antiangiogenic activity in HUVECs under hypoxic condition assessed as inhibition of tube formation 23153200
ACHN Cytotoxic Assay 6 d IC50=2.5 μM 23360104
A498 Cytotoxic Assay 100 μM 72 h DMSO IC50=4.3 μM 23489626
HUVEC Growth Inhibition Assay 3 μM 24 h DMSO Antiangiogenic activity assessed as inhibition of VEGF-induced tube formation with EC50 of 0.645 μM 23583911
HUVEC Kinase Assay 200 μM DMSO Inhibition of VEGFR2 phosphorylation in growth factor-stimulated HUVEC 23583911
HUVEC Kinase Assay 200 μM DMSO Inhibition of VEGFR1 phosphorylation in growth factor-stimulated HUVEC 23583911
A549 Cytotoxic Assay 72 h DMSO IC50=2.44 μM 23602441
HCT116 Cytotoxic Assay 72 h DMSO IC50=4.71 μM 23602441
MCF7 Cytotoxic Assay 72 h DMSO IC50=6.29 μM 23602441
BGC Growth Inhibition Assay 72 h DMSO IC50=4.78 μM 23999040
BxPC3 Growth Inhibition Assay 72 h DMSO IC50=3.63 μM 23999040
HT-29 Growth Inhibition Assay 72 h DMSO IC50=1.47 μM 23999040
T24 Growth Inhibition Assay 72 h DMSO IC50=2.44 μM 23999040
4T1 Cytotoxic Assay 72 h DMSO IC50=0.016 μM 24890652
MCF7 Cytotoxic Assay 72 h DMSO IC50=0.0271 μM 24890652
MCF7 Cytotoxic Assay 72 h DMSO IC50=0.0293 μM 24890652
MDA-MB-231 Cytotoxic Assay 72 h DMSO IC50=0.0223 μM 24890652
MDA-MB-435 Cytotoxic Assay 72 h DMSO IC50=0.0097 μM 24890652
MDA-MB-468 Cytotoxic Assay 72 h DMSO IC50=0.0061 μM 24890652
A431 Kinase Assay 10 μM 1 h DMSO Inhibition of EGFR with IC50 of 0.1721 μM 24890652
SH-SY5Y Kinase Assay 10 μM 1 h DMSO Inhibition of PDGFRbeta with IC50 of 0.0831 μM 24890652
U251 Kinase Assay 10 μM 1 h DMSO Inhibition of VEGFR2 with IC50 of 0.0189 μM 24890652
Bel7402 Growth Inhibition Assay 72 h DMSO IC50=2.67 μM 24904961
HK2 Growth Inhibition Assay 72 h DMSO IC50=5.85 μM 24904961
LO2 Growth Inhibition Assay 72 h DMSO IC50=19.93 μM 24904961
MV4-11 Growth Inhibition Assay 48 h DMSO IC50=0.003 μM 24904961
NCI-H3122 Growth Inhibition Assay 72 h DMSO IC50=0.83 μM 24904961
NCI-H460 Growth Inhibition Assay 72 h DMSO IC50=4.31 μM 24904961
NCI-H526 Growth Inhibition Assay 72 h DMSO IC50=1.01 μM 24904961
TT Growth Inhibition Assay 72 h DMSO IC50=0.04 μM 24904961
3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse 3T3 cells expressing human CSF1R after 72 hrs by Celltiter assay, Activity = 0.09 μM. 18694641
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay, IC50 = 0.0043 μM. 19754199
HEK293 Function assay Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd = 0.00047 μM. 19754199
FDC-P1 Function assay 48 hrs Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay, IC50 = 0.155 μM. 20156689
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM. 22221201
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay, IC50 = 0.03 μM. 22221201
primary leukemia cells Cytotoxicity assay 72 hrs Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay, IC50 = 1.1 μM. 22221201
endothelial precursor cells Function assay Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay, IC50 = 0.0096 μM. 22409666
endothelial precursor cells Function assay Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay, IC50 = 13.6 μM. 22409666
U251 Function assay 60 mins Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA, IC50 = 18.9 μM. 22739090
U251 Function assay 60 mins Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis, IC50 = 18.9 μM. 23375090
U251 Function assay 60 mins Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA, IC50 = 18.9 μM. 23434139
CHO Function assay Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50 = 33.4 μM. 23812503
U251 Function assay Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50 = 0.0189 μM. 24900865
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 10.5 μM. 25064347
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 13.6 μM. 25064347
CHO Function assay Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform, IC50 = 7.94328 μM. 25087753
CHO K1 Function assay Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform, IC50 = 10 μM. 25087753
CHO K1 Function assay Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 15.8489 μM. 25087753
HEK293 Function assay Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform, IC50 = 39.8107 μM. 25087753
MOLM13 Cytotoxicity assay 48 hrs Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0177 μM. 25089810
MV4-11 Cytotoxicity assay 48 hrs Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0243 μM. 25089810
HL60 Cytotoxicity assay 48 hrs Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0368 μM. 25089810
THP1 Cytotoxicity assay 48 hrs Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay, IC50 = 0.0457 μM. 25089810
ACHN Cytotoxicity assay 72 hrs Cytotoxicity against human ACHN cells after 72 hrs by MTT assay, IC50 = 2 μM. 25124114
U251 Function assay 60 min Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0189 μM. 25882519
U251 Function assay 60 min Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.0831 μM. 25882519
A431 Function assay 60 min Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method, IC50 = 0.1721 μM. 25882519
HT-29 Cytotoxicity assay 48 hrs Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 4.7 μM. 26009164
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 7.93 μM. 26009164
SKOV3 Cytotoxicity assay 48 hrs Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 9.21 μM. 26009164
PANC1 Cytotoxicity assay 48 hrs Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 14.94 μM. 26009164
HepG2 Cytotoxicity assay 48 hrs Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 16.06 μM. 26009164
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay, IC50 = 25.41 μM. 26009164
Bel7402 Photocytotoxicity assay 5 hrs Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 11 μM. 26584085
PANC1 Photocytotoxicity assay 5 hrs Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay, EC50 = 13 μM. 26584085
SVEC4-10 Cytotoxicity assay 24 hrs Cytotoxicity against mouse SVEC4-10 cells assessed as cell viability after 24 hrs by MTS assay, IC50 = 8 μM. 26912111
HUVEC Antiangiogenic assay 10 uM 5 hrs Antiangiogenic activity in human HUVEC cells assessed as angiogenesis rate at 10 uM after 5 hrs by endothelial tube formation assay relative to control 26912111
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 1.7 μM. 26920800
A549 Cytotoxicity assay Cytotoxicity against human A549 cells by MTT assay, IC50 = 9.1 μM. 26920800
MDA-MB-435 Cytotoxicity assay Cytotoxicity against human MDA-MB-435 cells by MTT assay, IC50 = 9.3 μM. 26920800
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM. 27077705
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.001 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.002 μM. 27077705
MOLM14 Antiproliferative assay 72 hrs Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.005 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.006 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.009 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.02 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.023 μM. 27077705
GISTT1 Antiproliferative assay 72 hrs Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.041 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.053 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.078 μM. 27077705
GIST882 Antiproliferative assay 72 hrs Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.11 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.51 μM. 27077705
Rec1 Antiproliferative assay 72 hrs Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 0.87 μM. 27077705
K562 Antiproliferative assay 72 hrs Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1 μM. 27077705
KU812 Antiproliferative assay 72 hrs Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.1 μM. 27077705
BCR-ABL dependent MEG01 Antiproliferative assay 72 hrs Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.2 μM. 27077705
BAF3 Function assay 72 hrs Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.38 μM. 27077705
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 1.7 μM. 27077705
GIST48B Antiproliferative assay 72 hrs Antiproliferative activity against human GIST48B cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.01 μM. 27077705
CHO Antiproliferative assay 72 hrs Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.03 μM. 27077705
CHL Antiproliferative assay 72 hrs Antiproliferative activity against CHL cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay, GI50 = 2.48 μM. 27077705
BAF3 Antiproliferative assay Antiproliferative activity against mouse BAF3 cells, GI50 = 2.78 μM. 27077705
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 7.4 μM. 27128173
BT549 Cytotoxicity assay 48 hrs Cytotoxicity against human BT549 cells after 48 hrs by MTT assay, IC50 = 15.5 μM. 27128173
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells after 48 hrs by MTT assay, IC50 = 16.4 μM. 27128173
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 19.6 μM. 27128173
RWPE1 Cytotoxicity assay 48 hrs Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay, IC50 = 23 μM. 27128173
MCF7 Function assay 1 uM 24 hrs Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated ERK1/2 at 1 uM incubated for 24 hrs by Western blot analysis 27176944
MCF7 Function assay 1 uM 24 hrs Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated Raf1 at 1 uM incubated for 24 hrs by Western blot analysis 27176944
PA1 Cytotoxicity assay 48 hrs Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 7.97 μM. 27210438
LNCAP Cytotoxicity assay 48 hrs Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 12.61 μM. 27210438
RWPE1 Cytotoxicity assay 48 hrs Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23 μM. 27210438
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 23.76 μM. 27210438
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 7.44 μM. 27448916
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 14.4 μM. 27448916
BT549 Cytotoxicity assay 48 hrs Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 15.54 μM. 27448916
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 16.38 μM. 27448916
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 19.6 μM. 27448916
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 23.8 μM. 27448916
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 7.4 μM. 27639369
HeLa Cytotoxicity assay 48 hrs Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 10.4 μM. 27639369
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 12.6 μM. 27639369
A549 Cytotoxicity assay 48 hrs Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 14.4 μM. 27639369
BT549 Cytotoxicity assay 48 hrs Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 15.5 μM. 27639369
DU145 Cytotoxicity assay 48 hrs Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 16.3 μM. 27639369
RWPE1 Cytotoxicity assay 48 hrs Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50 = 25.2 μM. 27639369
L02 Cytotoxicity assay 72 hrs Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay, IC50 = 4.62 μM. 27643639
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay, IC50 = 4.95 μM. 27643639
U251 Function assay 60 mins Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method, IC50 = 0.0189 μM. 27894589
SF539 Function assay 60 mins Inhibition of PDGFR-beta in human SF539 cells assessed as reduction in PDGF-BB induced phosphorylation preincubated for 60 mins followed by PDGF-BB addition measured after 10 mins by ELISA method, IC50 = 0.0831 μM. 27894589
HuH7 Growth inhibition assay 48 hrs Growth inhibition of human HuH7 cells after 48 hrs by MTT assay, IC50 = 3.03 μM. 27956344
HCT116 Growth inhibition assay 48 hrs Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50 = 5.62 μM. 27956344
SW620 Growth inhibition assay 48 hrs Growth inhibition of human SW620 cells after 48 hrs by MTT assay, IC50 = 6.25 μM. 27956344
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay, IC50 = 0.0385 μM. 28038328
CHO Function assay Inhibition of human ERG expressed in CHO cells by Qpatch assay, IC50 = 0.5 μM. 28038328
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 16.06 μM. 28057423
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 25.41 μM. 28057423
HEK293 Function assay 2 mins Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay, IC50 = 6.1 μM. 28230985
RCC4 Anticancer assay 48 hrs Anticancer activity against human RCC4 cells after 48 hrs by XTT assay, IC50 = 4 μM. 28325600
MDA-MB-231 Anticancer assay 48 hrs Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay, IC50 = 6 μM. 28325600
COLO205 Cytotoxicity assay 24 hrs Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay, IC50 = 8 μM. 28756024
K562 Cytotoxicity assay 24 hrs Cytotoxicity against human K562 cells after 24 hrs by MTT assay, IC50 = 14 μM. 28756024
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 32 μM. 28756024
MDA-MB-231 Cytotoxicity assay 24 hrs Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 6.98 μM. 28760313
MCF7 Function assay 4 uM 24 hrs Inhibition of VEGFR2 phosphorylation in human MCF7 cells at 4 uM incubated for 24 hrs by Western blot method 28942113
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.04 μM. 28991465
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.09 μM. 28991465
GIST430 Cytotoxicity assay 72 hrs Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.098 μM. 28991465
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 5.88 μM. 28991465
HuH7 Antiproliferative assay 48 hrs Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.707 μM. 29057042
A498 Antiproliferative assay 48 hrs Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 7.981 μM. 29057042
NCI-H727 Antiproliferative assay 48 hrs Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 10.12 μM. 29057042
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay, IC50 = 0.01 μM. 29935772
HuH7 Antiproliferative assay Antiproliferative activity against human HuH7 cells by MTT assay, IC50 = 3.03 μM. 30059803
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 5.62 μM. 30059803
SW620 Antiproliferative assay Antiproliferative activity against human SW620 cells by MTT assay, IC50 = 6.25 μM. 30059803
HepG2 Antiproliferative assay Antiproliferative activity against human HepG2 cells by MTT assay, IC50 = 7.78 μM. 30059803
U251 Function assay 60 mins Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA, IC50 = 0.0189 μM. 30098869
SH-SY5Y Function assay 60 mins Inhibition of PDGF-BB-induced PDGFRbeta activation in human SH-SY5Y cells pretreated for 60 mins followed by PDGF-BB addition and measured after 10 mins by ELISA, IC50 = 0.0831 μM. 30098869
A431 Function assay 60 mins Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA, IC50 = 0.1721 μM. 30098869
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.004 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.005 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.006 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.007 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.012 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.024 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.027 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.03 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.214 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.271 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.398 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.43 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.584 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.631 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.638 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.696 μM. 30204441
BA/F3 Function assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.782 μM. 30204441
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 4.789 μM. 30204441
Sf21 Function assay 60 mins Inhibition of recombinant human N-terminal His6-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells after 60 mins by ELISA, IC50 = 0.0047 μM. 30241010
EoL-1-cell Growth Inhibition Assay IC50=1.64 pM SANGER
MV-4-11 Growth Inhibition Assay IC50=272 pM SANGER
NOS-1 Growth Inhibition Assay IC50=15.3 nM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=30.94 nM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=33.8 nM SANGER
ALL-PO Growth Inhibition Assay IC50=79.89 nM SANGER
NKM-1 Growth Inhibition Assay IC50=98.52 nM SANGER
KM12 Growth Inhibition Assay IC50=350.14 nM SANGER
TE-15 Growth Inhibition Assay IC50=507.61 nM SANGER
697 Growth Inhibition Assay IC50=614.25 nM SANGER
MOLT-16 Growth Inhibition Assay IC50=631.32 nM SANGER
GB-1 Growth Inhibition Assay IC50=710.23 nM SANGER
TE-12 Growth Inhibition Assay IC50=804.55 nM SANGER
ES6 Growth Inhibition Assay IC50=981.06 nM SANGER
LC-2-ad Growth Inhibition Assay IC50=1.11407 μM SANGER
BL-70 Growth Inhibition Assay IC50=1.11846 μM SANGER
ETK-1 Growth Inhibition Assay IC50=1.2858 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=1.34141 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=1.36851 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=1.37009 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=1.46486 μM SANGER
PSN1 Growth Inhibition Assay IC50=1.50676 μM SANGER
SR Growth Inhibition Assay IC50=1.54572 μM SANGER
A3-KAW Growth Inhibition Assay IC50=1.62546 μM SANGER
KS-1 Growth Inhibition Assay IC50=1.69247 μM SANGER
CTV-1 Growth Inhibition Assay IC50=1.72751 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=1.81624 μM SANGER
EMG-01 Growth Inhibition Assay IC50=1.83563 μM SANGER
TE-11 Growth Inhibition Assay IC50=1.83985 μM SANGER
CMK Growth Inhibition Assay IC50=1.95517 μM SANGER
NB1 Growth Inhibition Assay IC50=1.96117 μM SANGER
HAL-01 Growth Inhibition Assay IC50=2.05946 μM SANGER
DEL Growth Inhibition Assay IC50=2.08482 μM SANGER
RL95-2 Growth Inhibition Assay IC50=2.11137 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=2.11313 μM SANGER
EW-16 Growth Inhibition Assay IC50=2.13508 μM SANGER
RS4-11 Growth Inhibition Assay IC50=2.17924 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=2.22375 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=2.33431 μM SANGER
RPMI-8402 Growth Inhibition Assay IC50=2.33618 μM SANGER
BV-173 Growth Inhibition Assay IC50=2.3366 μM SANGER
TE-10 Growth Inhibition Assay IC50=2.34384 μM SANGER
TE-8 Growth Inhibition Assay IC50=2.37038 μM SANGER
K052 Growth Inhibition Assay IC50=2.40202 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=2.49446 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=2.60237 μM SANGER
KGN Growth Inhibition Assay IC50=2.60339 μM SANGER
ML-2 Growth Inhibition Assay IC50=2.63512 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=2.69545 μM SANGER
LXF-289 Growth Inhibition Assay IC50=2.72989 μM SANGER
A101D Growth Inhibition Assay IC50=2.78304 μM SANGER
KY821 Growth Inhibition Assay IC50=2.79758 μM SANGER
ES4 Growth Inhibition Assay IC50=2.80628 μM SANGER
SCC-3 Growth Inhibition Assay IC50=2.82891 μM SANGER
NALM-6 Growth Inhibition Assay IC50=2.90473 μM SANGER
BL-41 Growth Inhibition Assay IC50=2.91222 μM SANGER
OPM-2 Growth Inhibition Assay IC50=3.05954 μM SANGER
SF126 Growth Inhibition Assay IC50=3.06198 μM SANGER
BE-13 Growth Inhibition Assay IC50=3.23111 μM SANGER
SF268 Growth Inhibition Assay IC50=3.32869 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=3.39838 μM SANGER
PF-382 Growth Inhibition Assay IC50=3.4457 μM SANGER
HEL Growth Inhibition Assay IC50=3.48005 μM SANGER
RPMI-6666 Growth Inhibition Assay IC50=3.54171 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=3.63391 μM SANGER
ATN-1 Growth Inhibition Assay IC50=3.67114 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=3.70508 μM SANGER
HCE-4 Growth Inhibition Assay IC50=3.78642 μM SANGER
SK-LMS-1 Growth Inhibition Assay IC50=3.83338 μM SANGER
MS-1 Growth Inhibition Assay IC50=3.83778 μM SANGER
JAR Growth Inhibition Assay IC50=3.98832 μM SANGER
KE-37 Growth Inhibition Assay IC50=4.06158 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=4.12168 μM SANGER
HH Growth Inhibition Assay IC50=4.20914 μM SANGER
HL-60 Growth Inhibition Assay IC50=4.21065 μM SANGER
HOP-62 Growth Inhibition Assay IC50=4.3352 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=4.33699 μM SANGER
DU-4475 Growth Inhibition Assay IC50=4.36729 μM SANGER
LC4-1 Growth Inhibition Assay IC50=4.3807 μM SANGER
MC116 Growth Inhibition Assay IC50=4.43081 μM SANGER
SW982 Growth Inhibition Assay IC50=4.55307 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=4.67099 μM SANGER
EW-1 Growth Inhibition Assay IC50=4.67911 μM SANGER
SU-DHL-1 Growth Inhibition Assay IC50=4.80174 μM SANGER
L-363 Growth Inhibition Assay IC50=4.80621 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=4.8731 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=5.17301 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=5.32312 μM SANGER
HC-1 Growth Inhibition Assay IC50=5.43291 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=5.4782 μM SANGER
SH-4 Growth Inhibition Assay IC50=5.4837 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=5.76719 μM SANGER
KG-1 Growth Inhibition Assay IC50=6.02878 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=6.07909 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=6.10949 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=6.12519 μM SANGER
SW954 Growth Inhibition Assay IC50=6.27517 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=6.32109 μM SANGER
ST486 Growth Inhibition Assay IC50=6.3471 μM SANGER
DG-75 Growth Inhibition Assay IC50=6.43069 μM SANGER
EW-3 Growth Inhibition Assay IC50=6.43207 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=6.51507 μM SANGER
GT3TKB Growth Inhibition Assay IC50=6.60763 μM SANGER
KU812 Growth Inhibition Assay IC50=6.6942 μM SANGER
CESS Growth Inhibition Assay IC50=7.10438 μM SANGER
BC-1 Growth Inhibition Assay IC50=7.24812 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=7.30389 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=7.3785 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=7.45804 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=7.50739 μM SANGER
ARH-77 Growth Inhibition Assay IC50=7.53597 μM SANGER
MN-60 Growth Inhibition Assay IC50=7.54088 μM SANGER
IMR-5 Growth Inhibition Assay IC50=7054876 μM SANGER
KARPAS-422 Growth Inhibition Assay IC50=7.57206 μM SANGER
CA46 Growth Inhibition Assay IC50=7.58012 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=7.66061 μM SANGER
no-11 Growth Inhibition Assay IC50=7.77557 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=8.02417 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=8.11652 μM SANGER
TALL-1 Growth Inhibition Assay IC50=8.18384 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=8.1942 μM SANGER
HCC1599 Growth Inhibition Assay IC50=8.19987 μM SANGER
CI-1 Growth Inhibition Assay IC50=8.20411 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=8.20661 μM SANGER
Daudi Growth Inhibition Assay IC50=8.23546 μM SANGER
CPC-N Growth Inhibition Assay IC50=8.29199 μM SANGER
MC-CAR Growth Inhibition Assay IC50=8.3358 μM SANGER
SW872 Growth Inhibition Assay IC50=8.34758 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=8.50351 μM SANGER
OCUB-M Growth Inhibition Assay IC50=8.56508 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=8.60985 μM SANGER
NCCIT Growth Inhibition Assay IC50=8.71745 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=9.13834 μM SANGER
COR-L279 Growth Inhibition Assay IC50=9.3909 μM SANGER
LS-123 Growth Inhibition Assay IC50=9.68161 μM SANGER
LP-1 Growth Inhibition Assay IC50=9.78083 μM SANGER
NB13 Growth Inhibition Assay IC50=9.79994 μM SANGER
ONS-76 Growth Inhibition Assay IC50=9.81016 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=9.99933 μM SANGER
GR-ST Growth Inhibition Assay IC50=10.2207 μM SANGER
ES1 Growth Inhibition Assay IC50=10.2984 μM SANGER
NB14 Growth Inhibition Assay IC50=10.9277 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=11.265 μM SANGER
RXF393 Growth Inhibition Assay IC50=11.4834 μM SANGER
NCI-H2107 Growth Inhibition Assay IC50=11.5984 μM SANGER
K562 Growth Inhibition Assay IC50=11.8702 μM SANGER
LOUCY Growth Inhibition Assay IC50=11.9875 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=12.002 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=12.1565 μM SANGER
K5 Growth Inhibition Assay IC50=12.2985 μM SANGER
BC-3 Growth Inhibition Assay IC50=12.4651 μM SANGER
REH Growth Inhibition Assay IC50=12.6498 μM SANGER
NEC8 Growth Inhibition Assay IC50=12.6887 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=12.8694 μM SANGER
NCI-H128 Growth Inhibition Assay IC50=13.0723 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=13.1144 μM SANGER
TGW Growth Inhibition Assay IC50=13.3276 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=13.345 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=13.6729 μM SANGER
CTB-1 Growth Inhibition Assay IC50=13.7294 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=13.7573 μM SANGER
LAN-6 Growth Inhibition Assay IC50=14.2457 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=14.2894 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=14.4169 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=14.5369 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=15.2251 μM SANGER
COR-L88 Growth Inhibition Assay IC50=16.0012 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=16.256 μM SANGER
KALS-1 Growth Inhibition Assay IC50=16.5931 μM SANGER
D-283MED Growth Inhibition Assay IC50=16.8489 μM SANGER
NCI-H719 Growth Inhibition Assay IC50=16.9161 μM SANGER
MLMA Growth Inhibition Assay IC50=16.9907 μM SANGER
EVSA-T Growth Inhibition Assay IC50=17.0485 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=17.6913 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=17.8572 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=17.9834 μM SANGER
A704 Growth Inhibition Assay IC50=17.9904 μM SANGER
L-428 Growth Inhibition Assay IC50=18.0151 μM SANGER
HCC1187 Growth Inhibition Assay IC50=18.0187 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=18.0866 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=18.4162 μM SANGER
EM-2 Growth Inhibition Assay IC50=18.5672 μM SANGER
Raji Growth Inhibition Assay IC50=19.9565 μM SANGER
TE-1 Growth Inhibition Assay IC50=20.4104 μM SANGER
SW962 Growth Inhibition Assay IC50=20.4293 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=20.5521 μM SANGER
no-10 Growth Inhibition Assay IC50=21.0264 μM SANGER
GDM-1 Growth Inhibition Assay IC50=21.9414 μM SANGER
KMS-12-PE Growth Inhibition Assay IC50=22.274 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=24.1278 μM SANGER
ES5 Growth Inhibition Assay IC50=24.7349 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=26.2742 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=27.1822 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=27.4946 μM SANGER
NB7 Growth Inhibition Assay IC50=27.9229 μM SANGER
A388 Growth Inhibition Assay IC50=28.0074 μM SANGER
JVM-2 Growth Inhibition Assay IC50=28.2898 μM SANGER
HT-144 Growth Inhibition Assay IC50=28.69 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=28.9195 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=29.0176 μM SANGER
EB-3 Growth Inhibition Assay IC50=29.5309 μM SANGER
KLE Growth Inhibition Assay IC50=29.619 μM SANGER
TK10 Growth Inhibition Assay IC50=30.126 μM SANGER
COLO-668 Growth Inhibition Assay IC50=30.792 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=31.1063 μM SANGER
GOTO Growth Inhibition Assay IC50=31.6085 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=31.8678 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=32.3843 μM SANGER
SCH Growth Inhibition Assay IC50=32.8485 μM SANGER
EHEB Growth Inhibition Assay IC50=34.1193 μM SANGER
U-266 Growth Inhibition Assay IC50=34.2781 μM SANGER
EW-11 Growth Inhibition Assay IC50=34.4725 μM SANGER
TE-9 Growth Inhibition Assay IC50=37.0401 μM SANGER
ES3 Growth Inhibition Assay IC50=37.5004 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=38.0843 μM SANGER
MPP-89 Growth Inhibition Assay IC50=42.0586 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=42.6405 μM SANGER
LC-1F Growth Inhibition Assay IC50=43.3682 μM SANGER
NH-12 Growth Inhibition Assay IC50=43.9359 μM SANGER
RKO Growth Inhibition Assay IC50=44.1252 μM SANGER
KM-H2 Growth Inhibition Assay IC50=44.9577 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=49.8825 μM SANGER
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (131.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

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% DMSO
%
% Tween 80
% ddH2O
% DMSO
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 532.56 Formula

C22H27FN4O2.C4H6O5

 Storage (From the date of receipt)
CAS No. 341031-54-7 Download SDF Storage of Stock Solutions

Synonyms SU11248 malate Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O

Mechanism of Action

Targets/IC50/Ki
IRE1α
Kit
(Cell-free assay)
FLT3
(Cell-free assay)
PDGFRβ
(Cell-free assay)
2 nM
VEGFR2
(Cell-free assay)
80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner.

Kinase Assay
Biochemical Tyrosine Kinase Assays
IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
In vivo

Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/14578466/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15304385/
  • [6] https://pubmed.ncbi.nlm.nih.gov/17041096/
  • [7] https://pubmed.ncbi.nlm.nih.gov/21317875/

Applications

Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK p-GSK3β / GSK3β / MYCN p-AKT / AKT / p-ERK / ERK
S1042-WB3
19244102
Growth inhibition assay Cell viability
S1042-viability1
24369536

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06222593 Not yet recruiting
Carcinoma Renal Cell
State University of New York at Buffalo
 June 1 2024 Phase 1|Phase 2
NCT06208748 Not yet recruiting
Gastrointestinal Stromal Tumors|GIST
Sarcoma Alliance for Research through Collaboration|Cogent Biosciences Inc.|Dana-Farber Cancer Institute|The Life Raft Group
 March 2024 Phase 2
NCT05745142 Completed
Carcinoma Renal Cell|Clear-cell Metastatic Renal Cell Carcinoma
Pfizer
 February 23 2023 --
NCT05043090 Recruiting
Papillary Renal Cell Carcinoma
AstraZeneca
 October 28 2021 Phase 3
NCT04669366 Completed
Kidney Neoplasms
Pfizer
 January 20 2021 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
I was wondering whether it is in its cis or trans form?

Answer:
It is Z form.

Question 2:
What is the difference between it (S1042) and Sunitinib (S7781)?

Answer:
S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same, but their solubility in aqueous solvent differs.

Signaling Pathway Map