Dasatinib Monohydrate

Synonyms: BMS-354825 Monohydrate

Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.

Dasatinib Monohydrate Chemical Structure

Dasatinib Monohydrate Chemical Structure

CAS: 863127-77-9

Selleck's Dasatinib Monohydrate has been cited by 236 publications

Purity & Quality Control

Batch: Purity: 99.62%
99.62

Dasatinib Monohydrate Related Products

Signaling Pathway

Choose Selective Src Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K562 cell Proliferation assay 72 h Antiproliferative activity against human K562 cells after 72 hrs, IC50=0.001 μM 15615512
WiDr cell Proliferation assay 72 h Antiproliferative activity against human WiDr cells after 72 hrs, IC50=0.052 μM 15615512
PC3 cell Proliferation assay 72 h Antiproliferative activity against human PC3 cells after 72 hrs, IC50=0.0094 μM 15615512
MDA-MB-231 cell Proliferation assay 72 h Antiproliferative activity against human MDA-MB-231 cells after 72 hrs, IC50=0.012 μM 15615512
M07ep210 cell Growth inhibition assay 48 h Growth inhibition of human M07ep210 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.07 nM 17956080
K562 cell Growth inhibition assay 48 h Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.001 μM 17956080
M07e cell Growth inhibition assay 48 h Growth inhibition of human M07e cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.0012 μM 17956080
K562 cell Cytotoxicity assay 72 h Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=12.83 μM 22217877
U937 cell Cytotoxicity assay 72 h Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=13.63 μM 22217877
K562 cell Proliferation assay 72 h Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50=0.7 nM 23521020
MDA-MB-435S cell Proliferation assay 72 h Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50=3.9 μM 23521020
NCI-H460 cell Proliferation assay 72 h Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50=8.99 μM 23521020
NCI-H23 cell Proliferation assay 72 h Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50=2.27 μM 23521020
A549 cell Proliferation assay 72 h Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=12.66 μM 23521020
T47D cell Proliferation assay 72 h Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50=0.9 μM 23521020
HCT116 cell Proliferation assay 72 h Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.3 μM 23521020
MCF7 cells Proliferation assay 72 h Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=2.57 μM 23521020
RXF 393NL cell Cytotoxicity assay 4 days Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining, IC50=21.7 nM 23253074
PRXF DU145 cell Cytotoxicity assay 4 days Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining, IC50=0.0623 μM 23253074
LXFA 983L cell Cytotoxicity assay 4 days Cytotoxicity against human LXFA 983L cells after 4 days by propidium iodide staining, IC50=56.5 nM 23253074
GXF251L cell Cytotoxicity assay 4 days Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining, IC50=2.25 μM 23253074
CXF 1103L cell Cytotoxicity assay 4 days Cytotoxicity against human CXF 1103L cells after 4 days by propidium iodide staining, IC50=4.36 μM 23253074
PAXF 1657L cell Cytotoxicity assay 4 days Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining, IC50=0.121 μM 23253074
NCI-H1648 cell Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.02011 μM SANGER
NCI-H1838 cell Growth inhibition assay Inhibition of human NCI-H1838 cell growth in a cell viability assay, IC50=1.30733 μM SANGER
NCI-H2126 cell Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=2.87552 μM SANGER
NCI-H2141 cell Growth inhibition assay Inhibition of human NCI-H2141 cell growth in a cell viability assay, IC50=24.7754 μM SANGER
NCI-H2107 cell Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=43.4847 μM SANGER
NCI-H747 cell Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.08362 μM SANGER
NCI-H720 cell Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=20.2733 μM SANGER
NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay.IC50=1.30859 μM SANGER
NMC-G1 cell Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay.IC50=0.11606 μM SANGER
NTERA-S-cl-D1 cell Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.IC50=0.12283 μM SANGER
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay.IC50=5.86154 μM SANGER
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay.IC50=1.04412 μM SANGER
OPM-2 cell Growth inhibition assay Inhibition of human OPM-2 cell growth in a cell viability assay.IC50=4.27685 μM SANGER
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay.IC50=0.0203 μM SANGER
ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay.IC50=0.42951 μM SANGER
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay.IC50=0.37433 μM SANGER
NCI-H446 cell Growth inhibition assay Inhibition of human NCI-H446 cell growth in a cell viability assay.IC50=0.6276 μM SANGER
NCI-H510A cell Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay.IC50=19.3973 μM SANGER
PF-382 cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay.IC50=0.17678 μM SANGER
NCI-H64 cell Growth inhibition assay Inhibition of human NCI-H64 cell growth in a cell viability assay.IC50=29.6253 μM SANGER
PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay.IC50=0.04474 μM SANGER
QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay.IC50=0.70629 μM SANGER
RL95-2 cell Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay.IC50=0.1038 μM SANGER
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay.IC50=0.4911 μM SANGER
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay.IC50=0.52966 μM SANGER
NCI-SNU-16 cell Growth inhibition assay Inhibition of human NCI-SNU-16 cell growth in a cell viability assay.IC50=8.56128 μM SANGER
RPMI-6666 cell Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay.IC50=7.27067 μM SANGER
NEC8 cell Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay.IC50=44.336 μM SANGER
RS4-11 cell Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay.IC50=7.65787 μM SANGER
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay.IC50=0.02357 μM SANGER
Raji cell Growth inhibition assay Inhibition of human Raji cell growth in a cell viability assay.IC50=13.7497 μM SANGER
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay.IC50=0.006129 μM SANGER
SBC-1 cell Growth inhibition assay Inhibition of human SBC-1 cell growth in a cell viability assay.IC50=1.57984 μM SANGER
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay.IC50=0.3541 μM SANGER
SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay.IC50=13.8557 μM SANGER
SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay.IC50=0.18413 μM SANGER
OMC-1 cell Growth inhibition assay Inhibition of human OMC-1 cell growth in a cell viability assay.IC50=27.1422 μM SANGER
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay.IC50=9.02493 μM SANGER
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay.IC50=8.72805 μM SANGER
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay.IC50=3.11886 μM SANGER
SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay.IC50=8.89155 μM SANGER
SKM-1 cell Growth inhibition assay Inhibition of human SKM-1 cell growth in a cell viability assay.IC50=9.01734 μM SANGER
SK-PN-DW cell Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay.IC50=36.1943 μM SANGER
SK-UT-1 cell Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay.IC50=2.16693 μM SANGER
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay.IC50=0.04435 μM SANGER
REH cell Growth inhibition assay Inhibition of human REH cell growth in a cell viability assay.IC50=20.6357 μM SANGER
SNU-C2B cell Growth inhibition assay Inhibition of human SNU-C2B cell growth in a cell viability assay.IC50=1.30589 μM SANGER
RPMI-8866 cell Growth inhibition assay Inhibition of human RPMI-8866 cell growth in a cell viability assay.IC50=17.4455 μM SANGER
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay.IC50=0.04161 μM SANGER
SW962 cell Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay.IC50=0.11292 μM SANGER
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay.IC50=0.17404 μM SANGER
TE-1 cell Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay.IC50=0.1054 μM SANGER
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay.IC50=0.15458 μM SANGER
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay.IC50=1.03043 μM SANGER
A253 cell Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay.IC50=3.73246 μM SANGER
A3-KAW cell Growth inhibition assay Inhibition of human A3-KAW cell growth in a cell viability assay.IC50=0.98452 μM SANGER
A4-Fuk cell Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay.IC50=38.1009 μM SANGER
A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay.IC50=0.05095 μM SANGER
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay.IC50=1.82252 μM SANGER
A704 cell Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay.IC50=0.01491 μM SANGER
ALL-PO cell Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay.IC50=10.7938 μM SANGER
ARH-77 cell Growth inhibition assay Inhibition of human ARH-77 cell growth in a cell viability assay.IC50=3.46915 μM SANGER
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay.IC50=4.49954 μM SANGER
BB65-RCC cell Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay.IC50=0.08227 μM SANGER
BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay.IC50=0.38599 μM SANGER
BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay.IC50=28.651 μM SANGER
BC-3 cell Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay.IC50=12.1138 μM SANGER
BL-41 cell Growth inhibition assay Inhibition of human BL-41 cell growth in a cell viability assay.IC50=0.29123 μM SANGER
BL-70 cell Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay.IC50=0.0000008218 μM SANGER
SW684 cell Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay.IC50=0.3498 μM SANGER
BOKU cell Growth inhibition assay Inhibition of human BOKU cell growth in a cell viability assay.IC50=0.49133 μM SANGER
SW954 cell Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay.IC50=0.02927 μM SANGER
C2BBe1 cell Growth inhibition assay Inhibition of human C2BBe1 cell growth in a cell viability assay.IC50=0.08308 μM SANGER
BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay.IC50=0.000000109 μM SANGER
Becker cell Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay.IC50=0.03003 μM SANGER
SW982 cell Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay.IC50=0.01115 μM SANGER
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay.IC50=0.19987 μM SANGER
TE-15 cell Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay.IC50=0.005891 μM SANGER
TE-11 cell Growth inhibition assay Inhibition of human TE-11 cell growth in a cell viability assay.IC50=0.07858 μM SANGER
TE-5 cell Growth inhibition assay Inhibition of human TE-5 cell growth in a cell viability assay.IC50=1.79139 μM SANGER
TE-6 cell Growth inhibition assay Inhibition of human TE-6 cell growth in a cell viability assay.IC50=1.21226 μM SANGER
TE-9 cell Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay.IC50=0.87532 μM SANGER
TGBC24TKB cell Growth inhibition assay Inhibition of human TGBC24TKB cell growth in a cell viability assay.IC50=0.04761 μM SANGER
TGW cell Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay.IC50=11.2828 μM SANGER
TK10 cell Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay.IC50=0.01174 μM SANGER
TGBC1TKB cell Growth inhibition assay Inhibition of human TGBC1TKB cell growth in a cell viability assay.IC50=0.06164 μM SANGER
A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay.IC50=0.07284 μM SANGER
UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay.IC50=12.9198 μM SANGER
U-87-MG cell Growth inhibition assay Inhibition of human U-87-MG cell growth in a cell viability assay.IC50=30.766 μM SANGER
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay.IC50=0.05437 μM SANGER
no-10 cell Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay.IC50=0.31931 μM SANGER
CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay.IC50=1.40992 μM SANGER
CGTH-W-1 cell Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay.IC50=0.03548 μM SANGER
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay.IC50=0.06357 μM SANGER
COLO-684 cell Growth inhibition assay Inhibition of human COLO-684 cell growth in a cell viability assay.IC50=46.2258 μM SANGER
TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay.IC50=0.01861 μM SANGER
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay.IC50=40.2852 μM SANGER
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay.IC50=0.01576 μM SANGER
CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay.IC50=0.19531 μM SANGER
CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay.IC50=0.00004036 μM SANGER
VA-ES-BJ cell Growth inhibition assay Inhibition of human VA-ES-BJ cell growth in a cell viability assay.IC50=0.03902 μM SANGER
D-263MG cell Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay.IC50=0.36224 μM SANGER
D-336MG cell Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay.IC50=0.006298 μM SANGER
D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay.IC50=1.23376 μM SANGER
DJM-1 cell Growth inhibition assay Inhibition of human DJM-1 cell growth in a cell viability assay.IC50=6.48558 μM SANGER
no-11 cell Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay.IC50=0.50228 μM SANGER
DMS-153 cell Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay.IC50=14.0028 μM SANGER
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay.IC50=0.24001 μM SANGER
DU-4475 cell Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay.IC50=8.21652 μM SANGER
EB-3 cell Growth inhibition assay Inhibition of human EB-3 cell growth in a cell viability assay.IC50=34.3118 μM SANGER
EHEB cell Growth inhibition assay Inhibition of human EHEB cell growth in a cell viability assay.IC50=10.0656 μM SANGER
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay.IC50=0.12213 μM SANGER
CP67-MEL cell Growth inhibition assay Inhibition of human CP67-MEL cell growth in a cell viability assay.IC50=0.20488 μM SANGER
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay.IC50=32.1252 μM SANGER
EVSA-T cell Growth inhibition assay Inhibition of human EVSA-T cell growth in a cell viability assay.IC50=9.27793 μM SANGER
ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay.IC50=1.05145 μM SANGER
ETK-1 cell Growth inhibition assay Inhibition of human ETK-1 cell growth in a cell viability assay.IC50=0.02832 μM SANGER
ES6 cell Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay.IC50=0.03193 μM SANGER
EW-24 cell Growth inhibition assay Inhibition of human EW-24 cell growth in a cell viability assay.IC50=0.78165 μM SANGER
EoL-1-cell cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay.IC50=0.00001309 μM SANGER
Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay.IC50=3.05741 μM SANGER
GAK cell Growth inhibition assay Inhibition of human GAK cell growth in a cell viability assay.IC50=31.2686 μM SANGER
D-247MG cell Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay.IC50=6.12519 μM SANGER
GB-1 cell Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay.IC50=0.02157 μM SANGER
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay.IC50=0.06118 μM SANGER
GCIY cell Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay.IC50=0.09656 μM SANGER
GT3TKB cell Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay.IC50=9.35546 μM SANGER
HC-1 cell Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay.IC50=24.5551 μM SANGER
HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay.IC50=19.7543 μM SANGER
HCC1187 cell Growth inhibition assay Inhibition of human HCC1187 cell growth in a cell viability assay.IC50=35.8052 μM SANGER
DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay.IC50=41.9086 μM SANGER
HCC1599 cell Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay.IC50=32.3325 μM SANGER
DOHH-2 cell Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay.IC50=0.01719 μM SANGER
HCC2157 cell Growth inhibition assay Inhibition of human HCC2157 cell growth in a cell viability assay.IC50=37.9946 μM SANGER
HCE-4 cell Growth inhibition assay Inhibition of human HCE-4 cell growth in a cell viability assay.IC50=0.26439 μM SANGER
HCE-T cell Growth inhibition assay Inhibition of human HCE-T cell growth in a cell viability assay.IC50=1.56714 μM SANGER
HEL cell Growth inhibition assay Inhibition of human HEL cell growth in a cell viability assay.IC50=10.4776 μM SANGER
EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay.IC50=0.000001078 μM SANGER
HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay.IC50=0.53609 μM SANGER
EW-16 cell Growth inhibition assay Inhibition of human EW-16 cell growth in a cell viability assay.IC50=0.76178 μM SANGER
IA-LM cell Growth inhibition assay Inhibition of human IA-LM cell growth in a cell viability assay.IC50=12.4445 μM SANGER
IST-MEL1 cell Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay.IC50=0.1345 μM SANGER
IST-MES1 cell Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay.IC50=0.08552 μM SANGER
GI-1 cell Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay.IC50=1.3622 μM SANGER
IST-SL2 cell Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay.IC50=0.50302 μM SANGER
JVM-2 cell Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay.IC50=2.36284 μM SANGER
JVM-3 cell Growth inhibition assay Inhibition of human JVM-3 cell growth in a cell viability assay.IC50=37.2338 μM SANGER
KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay.IC50=0.0949 μM SANGER
KARPAS-422 cell Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay.IC50=0.33997 μM SANGER
JiyoyeP-2003 cell Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay.IC50=1.73466 μM SANGER
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay.IC50=7.51671 μM SANGER
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay.IC50=0.01942 μM SANGER
KLE cell Growth inhibition assay Inhibition of human KLE cell growth in a cell viability assay.IC50=0.11317 μM SANGER
KNS-42 cell Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay.IC50=1.24412 μM SANGER
KNS-81-FD cell Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay.IC50=23.146 μM SANGER
KP-N-YS cell Growth inhibition assay Inhibition of human KP-N-YS cell growth in a cell viability assay.IC50=12.9283 μM SANGER
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay.IC50=0.01834 μM SANGER
KURAMOCHI cell Growth inhibition assay Inhibition of human KURAMOCHI cell growth in a cell viability assay.IC50=0.03487 μM SANGER
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay.IC50=0.3142 μM SANGER
LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay.IC50=0.000003207 μM SANGER
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay.IC50=0.009887 μM SANGER
LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay.IC50=0.14162 μM SANGER
LB373-MEL-D cell Growth inhibition assay Inhibition of human LB373-MEL-D cell growth in a cell viability assay.IC50=0.82508 μM SANGER
LB771-HNC cell Growth inhibition assay Inhibition of human LB771-HNC cell growth in a cell viability assay.IC50=2.57551 μM SANGER
LB996-RCC cell Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay.IC50=0.009912 μM SANGER
LC-2-ad cell Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay.IC50=0.02586 μM SANGER
J-RT3-T3-5 cell Growth inhibition assay Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay.IC50=8.96529 μM SANGER
LP-1 cell Growth inhibition assay Inhibition of human LP-1 cell growth in a cell viability assay.IC50=7.54782 μM SANGER
K-562 cell Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay.IC50=0.0000002656 μM SANGER
LS-123 cell Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay.IC50=0.14064 μM SANGER
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay.IC50=0.16489 μM SANGER
LS-411N cell Growth inhibition assay Inhibition of human LS-411N cell growth in a cell viability assay.IC50=48.4748 μM SANGER
KG-1 cell Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay.IC50=4.60845 μM SANGER
KINGS-1 cell Growth inhibition assay Inhibition of human KINGS-1 cell growth in a cell viability assay.IC50=0.16666 μM SANGER
LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay.IC50=0.03956 μM SANGER
MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay.IC50=0.1141 μM SANGER
KS-1 cell Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay.IC50=0.0273 μM SANGER
KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay.IC50=0.11883 μM SANGER
MEG-01 cell Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay.IC50=0.000009805 μM SANGER
MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay.IC50=0.04724 μM SANGER
L-540 cell Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay.IC50=15.0671 μM SANGER
MHH-NB-11 cell Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay.IC50=43.0818 μM SANGER
MMAC-SF cell Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay.IC50=8.79307 μM SANGER
LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay.IC50=9.02012 μM SANGER
LB831-BLC cell Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay.IC50=0.04609 μM SANGER
MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay.IC50=29.6292 μM SANGER
LC-1F cell Growth inhibition assay Inhibition of human LC-1F cell growth in a cell viability assay.IC50=27.3245 μM SANGER
MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay.IC50=26.6753 μM SANGER
MZ1-PC cell Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay.IC50=0.03119 μM SANGER
MONO-MAC-6 cell Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay.IC50=8.27066 μM SANGER
MZ2-MEL cell Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay.IC50=0.28537 μM SANGER
MPP-89 cell Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay.IC50=0.04049 μM SANGER
MZ7-mel cell Growth inhibition assay Inhibition of human MZ7-mel cell growth in a cell viability assay.IC50=0.47911 μM SANGER
LOXIMVI cell Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay.IC50=0.31503 μM SANGER
NALM-6 cell Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay.IC50=0.19295 μM SANGER
NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay.IC50=19.4877 μM SANGER
NB5 cell Growth inhibition assay Inhibition of human NB5 cell growth in a cell viability assay.IC50=1.39827 μM SANGER
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay.IC50=3.63847 μM SANGER
NCCIT cell Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay.IC50=2.86616 μM SANGER
NB69 cell Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay.IC50=0.14436 μM SANGER
NCI-H1304 cell Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay.IC50=28.1628 μM SANGER
NCI-H1395 cell Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay.IC50=42.0163 μM SANGER
MHH-PREB-1 cell Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay.IC50=0.74469 μM SANGER
MLMA cell Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay.IC50=0.14032 μM SANGER
MN-60 cell Growth inhibition assay Inhibition of human MN-60 cell growth in a cell viability assay.IC50=15.1979 μM SANGER
MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay.IC50=4.36454 μM SANGER
NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay.IC50=9.92259 μM SANGER
NCI-H1355 cell Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay.IC50=0.11028 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
Targets
Abl [1]
(Cell-free assay)
Src [1]
(Cell-free assay)
c-Kit (D816V) [2]
(Cell-free assay)
c-Kit (wt) [2]
(Cell-free assay)
0.6 nM 0.8 nM 37 nM 79 nM
In vitro
In vitro Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. Dasatinib has a two-log (∼325-fold) increased potency relative to imatinib. Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range. Dasatinib directly targets wild-type and mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl. [1] The percent of colonies of TgE bone marrow cells are decreased from 100% in untreated wells to 4.12% in Dasatinib treated wells. In the presence of Dasatinib, the difference in the percentage of colonies formed by WT and TgE bone marrow cells is statistically significant. Expression of LMP2A is able to promote B lymphocyte survival and proliferation, which can be inhibited by targeting Lyn and/or c-Abl kinases through Dasatinib. [3] Dasatinib treatment inhibits Src signaling, decreases growth, and induces cell cycle arrest and apoptosis in a subset of thyroid cancer cells. Treatment with increasing doses of Dasatinib (0.019 μM to 1.25 μM) for 3 days inhibits the growth of the C643, TPC1, BCPAP, and SW1736 cell lines by about 50% at low nanomolar concentrations, while higher concentrations are required to inhibit the growth of the K1 cell line. Treatment with 10 nM or 50 nM Dasatinib results in a 9-22% increase of cells in the G1 population among BCPAP and SW1736 and K1 cells, and a corresponding 7-18% decrease in the percentage of cells in the S phase. [4]
Kinase Assay Kinase autophosphorylation assays
Kinase assays using wild-type and mutant glutathione S-transferase (GST)-Abl fusion proteins (c-Abl amino acids 220-498) are done. GST-Abl fusion proteins are released from glutathione-Sepharose beads before use; the concentration of ATP is 5 μM. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase. After 1-hour incubation at 30 °C, LAR phosphatase is inactivated by addition of sodium vanadate (1 mM). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase is routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The Dasatinib concentration range is extended to 1,000 nM for mutant T315I. These same inhibitor concentrations are used for the in vitro peptide substrate phosphorylation assays. The three inhibitors are tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase.
Cell Research Cell lines Ba/F3 cell lines
Concentrations ~32 nM
Incubation Time 72 hours
Method

Ba/F3 cell lines are seeded in triplicate and incubated with escalating concentrations of Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges are 0 nM to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 200 nM for mutant T315I.

Experimental Result Images Methods Biomarkers Images PMID
Western blot phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 cleaved caspase 3 p-FAK/p-STAT3 23049975
Growth inhibition assay Cell viability 23721490
Immunofluorescence SRC / Met α-tubulin F-actin / Actinin-4 / Paxillin 26517812
ELISA TNF-α E-selectin VCAM-1 17684099
In Vivo
In vivo Dasatinib reverses splenomegaly in LMP2A/MYC double transgenic mice. Dasatinib specifically prevents colony formation by LMP2A expressing bone marrow B cells and decreased spleen size in the TgE mice. Spleen mass is significantly decreased among Dasatinib treated Tg6/λ-MYC mice when compared to the control group. Dasatinib inhibits lymphadenopathy in LMP2A/MYC double transgenic mice. Dasatinib reverses splenomegaly in Rag1KO mice engrafted with tumor cells from LMP2A/MYC double transgenic mice. Dasatinib therapy inhibits Lyn phosphorylation in B lymphocyte tumors expressing LMP2A. [3]
Animal Research Animal Models EμLMP2A (TgE and Tg6 strains), MYC (λ-MYC), and LMP2A/λ-MYC double transgenic mice (Tg6/λ-MYC)
Dosages 30 mg/kg
Administration Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05527418 Not yet recruiting
Recent HIV-1 Infection
Eva Bonfill|Institut d''Investigacions Biomèdiques August Pi i Sunyer
November 2023 Phase 2
NCT05993949 Recruiting
Lymphoblastic Leukemia
Stanford University|Kite Pharma
October 2 2023 Phase 1
NCT05780073 Recruiting
HIV Infection Primary
Fundació Institut Germans Trias i Pujol|Fundación FLS de Lucha Contra el Sida Enfermedades Infecciosas y Promoción de la Salud y Ciencia|Spanish Clinical Research Network - SCReN|IrsiCaixa|University of Turin Italy|Instituto de Salud Carlos III|Germans Trias i Pujol Hospital
October 16 2023 Phase 2
NCT05198843 Terminated
Anatomic Stage IV Breast Cancer AJCC v8|Metastatic Triple-Negative Breast Inflammatory Carcinoma
National Cancer Institute (NCI)
November 8 2022 Phase 1|Phase 2
NCT04925648 Recruiting
Metastatic Prostate Cancer
St Vincent''s Hospital Sydney
October 18 2021 Phase 2

Chemical Information & Solubility

Molecular Weight 506.02 Formula

C22H28ClN7O3S

CAS No. 863127-77-9 SDF Download Dasatinib Monohydrate SDF
Smiles CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (197.62 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What’s the difference between S1021 and S7782?

Answer:
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than hydrate one (S7782).

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