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Pazopanib VEGFR inhibitor

Name: Pazopanib
Brand: Selleck Chemicals
SKU: S3012
Availability: InStock
Rating: 5 (83 reviews)

Cat.No.S3012

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. This compound induces cathepsin B activation and autophagy.

Chemical Structure

Molecular Weight: 437.52

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other VEGFR Inhibitors	SAR131675 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Linifanib (ABT-869) Anlotinib (AL3818) Dihydrochloride Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl Semaxanib (SU5416)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human HT29 cells	Proliferation assay			Antiproliferative activity against human HT29 cells in serum containing medium	18620382
human A375P cells	Proliferation assay			Antiproliferative activity against human A375P cells in serum containing medium	18620382
human HN5 cells	Proliferation assay			Antiproliferative activity against human HN5 cells in serum containing medium	18620382
HUVEC	Function assay	1 μM	6 h	Antiangiogenic activity in HUVEC assessed as inhibition of tube formation at 0.1 uM after 6 hrs by Matrigel assay	24036042
HT-29	Function assay		14 to 24 hrs	Inhibition of RIPK1 in human HT-29 cells assessed as reduction in TNFalpha-induced necroptosis incubated for 14 to 24 hrs in presence of Smac mimetic and z-VAD-FMK by cell titer glo-based luminescence assay, IC50=0.873μM	31622096
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
HUVEC	Function assay	100 nM	2 hrs	Inhibition of VEGF-stimulated VEGFR2 phosphorylation in human HUVEC cells at 100 nM preincubated for 2 hrs followed by VEGF stimulation by Western blot analysis	29787262
HUVEC	Antiangiogenic assay	0.1 uM	6 hrs	Antiangiogenic activity in human HUVEC cells assessed as reduction in capillary-like tubular network formation at 0.1 uM after 6 hrs by phase-contrast microscopy	29787262
EoL-1-cell	Growth inhibition assay			Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000289μM	SANGER
AN3-CA	Growth inhibition assay			Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=0.01005μM	SANGER
CGTH-W-1	Growth inhibition assay			Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=0.04001μM	SANGER
GDM-1	Growth inhibition assay			Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.10399μM	SANGER
A204	Growth inhibition assay			Inhibition of human A204 cell growth in a cell viability assay, IC50=0.10906μM	SANGER
G-402	Growth inhibition assay			Inhibition of human G-402 cell growth in a cell viability assay, IC50=0.53184μM	SANGER
MFE-296	Growth inhibition assay			Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=0.59022μM	SANGER
NOS-1	Growth inhibition assay			Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.65987μM	SANGER
KG-1	Growth inhibition assay			Inhibition of human KG-1 cell growth in a cell viability assay, IC50=0.71755μM	SANGER
HT55	Growth inhibition assay			Inhibition of human HT55 cell growth in a cell viability assay, IC50=0.98781μM	SANGER
MG-63	Growth inhibition assay			Inhibition of human MG-63 cell growth in a cell viability assay, IC50=1.00146μM	SANGER
CCF-STTG1	Growth inhibition assay			Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.04981μM	SANGER
RT-112	Growth inhibition assay			Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.10376μM	SANGER
MC-IXC	Growth inhibition assay			Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=1.11512μM	SANGER
HUTU-80	Growth inhibition assay			Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.28103μM	SANGER
MV-4-11	Growth inhibition assay			Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=1.34501μM	SANGER
LCLC-103H	Growth inhibition assay			Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=1.44549μM	SANGER
G-401	Growth inhibition assay			Inhibition of human G-401 cell growth in a cell viability assay, IC50=1.46421μM	SANGER
A704	Growth inhibition assay			Inhibition of human A704 cell growth in a cell viability assay, IC50=1.60323μM	SANGER
ESS-1	Growth inhibition assay			Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=1.60396μM	SANGER
HLE	Growth inhibition assay			Inhibition of human HLE cell growth in a cell viability assay, IC50=1.63804μM	SANGER
NY	Growth inhibition assay			Inhibition of human NY cell growth in a cell viability assay, IC50=1.84821μM	SANGER
A427	Growth inhibition assay			Inhibition of human A427 cell growth in a cell viability assay, IC50=1.98075μM	SANGER
SK-N-DZ	Growth inhibition assay			Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=2.02381μM	SANGER
J82	Growth inhibition assay			Inhibition of human J82 cell growth in a cell viability assay, IC50=2.06088μM	SANGER
GI-1	Growth inhibition assay			Inhibition of human GI-1 cell growth in a cell viability assay, IC50=2.22951μM	SANGER
NCI-H716	Growth inhibition assay			Inhibition of human NCI-H716 cell growth in a cell viability assay, IC50=2.31633μM	SANGER
SF126	Growth inhibition assay			Inhibition of human SF126 cell growth in a cell viability assay, IC50=2.47459μM	SANGER
H4	Growth inhibition assay			Inhibition of human H4 cell growth in a cell viability assay, IC50=2.51262μM	SANGER
LB831-BLC	Growth inhibition assay			Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=2.54566μM	SANGER
HCC1395	Growth inhibition assay			Inhibition of human HCC1395 cell growth in a cell viability assay, IC50=2.58156μM	SANGER
LK-2	Growth inhibition assay			Inhibition of human LK-2 cell growth in a cell viability assay, IC50=2.64569μM	SANGER
G-361	Growth inhibition assay			Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.04082μM	SANGER
NCI-H2342	Growth inhibition assay			Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=3.13316μM	SANGER
SK-LU-1	Growth inhibition assay			Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.18767μM	SANGER
IGROV-1	Growth inhibition assay			Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=3.24713μM	SANGER
EB2	Growth inhibition assay			Inhibition of human EB2 cell growth in a cell viability assay, IC50=3.28168μM	SANGER
CAL-54	Growth inhibition assay			Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=3.28367μM	SANGER
OCUB-M	Growth inhibition assay			Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=3.31368μM	SANGER
LB1047-RCC	Growth inhibition assay			Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=3.53164μM	SANGER
Daudi	Growth inhibition assay			Inhibition of human Daudi cell growth in a cell viability assay, IC50=3.66219μM	SANGER
A172	Growth inhibition assay			Inhibition of human A172 cell growth in a cell viability assay, IC50=3.7379μM	SANGER
KGN	Growth inhibition assay			Inhibition of human KGN cell growth in a cell viability assay, IC50=4.06709μM	SANGER
SNG-M	Growth inhibition assay			Inhibition of human SNG-M cell growth in a cell viability assay, IC50=4.08669μM	SANGER
SW1710	Growth inhibition assay			Inhibition of human SW1710 cell growth in a cell viability assay, IC50=4.47318μM	SANGER
Daoy	Growth inhibition assay			Inhibition of human Daoy cell growth in a cell viability assay, IC50=4.77949μM	SANGER
DMS-273	Growth inhibition assay			Inhibition of human DMS-273 cell growth in a cell viability assay, IC50=4.96202μM	SANGER
KU812	Growth inhibition assay			Inhibition of human KU812 cell growth in a cell viability assay, IC50=5.37812μM	SANGER
NCI-H727	Growth inhibition assay			Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50=5.40901μM	SANGER
P30-OHK	Growth inhibition assay			Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=5.4694μM	SANGER
MIA-PaCa-2	Growth inhibition assay			Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50=5.60466μM	SANGER
TT	Growth inhibition assay			Inhibition of human TT cell growth in a cell viability assay, IC50=5.6624μM	SANGER
DK-MG	Growth inhibition assay			Inhibition of human DK-MG cell growth in a cell viability assay, IC50=5.72028μM	SANGER
GB-1	Growth inhibition assay			Inhibition of human GB-1 cell growth in a cell viability assay, IC50=5.73434μM	SANGER
NCI-H520	Growth inhibition assay			Inhibition of human NCI-H520 cell growth in a cell viability assay, IC50=5.73435μM	SANGER
WM-115	Growth inhibition assay			Inhibition of human WM-115 cell growth in a cell viability assay, IC50=5.75644μM	SANGER
CAL-72	Growth inhibition assay			Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=5.9381μM	SANGER
NCI-H1573	Growth inhibition assay			Inhibition of human NCI-H1573 cell growth in a cell viability assay, IC50=5.96542μM	SANGER
ES6	Growth inhibition assay			Inhibition of human ES6 cell growth in a cell viability assay, IC50=6.02688μM	SANGER
TE-8	Growth inhibition assay			Inhibition of human TE-8 cell growth in a cell viability assay, IC50=6.16473μM	SANGER
GAMG	Growth inhibition assay			Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.17776μM	SANGER
HGC-27	Growth inhibition assay			Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=6.2015μM	SANGER
CTV-1	Growth inhibition assay			Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=6.20903μM	SANGER
NCI-H810	Growth inhibition assay			Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=6.31365μM	SANGER
NMC-G1	Growth inhibition assay			Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=6.55237μM	SANGER
SNB75	Growth inhibition assay			Inhibition of human SNB75 cell growth in a cell viability assay, IC50=6.56939μM	SANGER
SK-MES-1	Growth inhibition assay			Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=6.8663μM	SANGER
MZ2-MEL	Growth inhibition assay			Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=6.93016μM	SANGER
TE-15	Growth inhibition assay			Inhibition of human TE-15 cell growth in a cell viability assay, IC50=7.16924μM	SANGER
S-117	Growth inhibition assay			Inhibition of human S-117 cell growth in a cell viability assay, IC50=7.57924μM	SANGER
HuH-7	Growth inhibition assay			Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=7.69384μM	SANGER
CAS-1	Growth inhibition assay			Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=7.76339μM	SANGER
D-502MG	Growth inhibition assay			Inhibition of human D-502MG cell growth in a cell viability assay, IC50=7.78222μM	SANGER
IA-LM	Growth inhibition assay			Inhibition of human IA-LM cell growth in a cell viability assay, IC50=7.93364μM	SANGER
CAKI-1	Growth inhibition assay			Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=8.28831μM	SANGER
KYSE-70	Growth inhibition assay			Inhibition of human KYSE-70 cell growth in a cell viability assay, IC50=8.45447μM	SANGER
HCC1569	Growth inhibition assay			Inhibition of human HCC1569 cell growth in a cell viability assay, IC50=8.46556μM	SANGER
SR	Growth inhibition assay			Inhibition of human SR cell growth in a cell viability assay, IC50=8.70202μM	SANGER
SH-4	Growth inhibition assay			Inhibition of human SH-4 cell growth in a cell viability assay, IC50=8.73653μM	SANGER
SW954	Growth inhibition assay			Inhibition of human SW954 cell growth in a cell viability assay, IC50=8.75347μM	SANGER
MPP-89	Growth inhibition assay			Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=8.7782μM	SANGER
IST-MEL1	Growth inhibition assay			Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=8.91086μM	SANGER
EFM-19	Growth inhibition assay			Inhibition of human EFM-19 cell growth in a cell viability assay, IC50=8.92276μM	SANGER
KS-1	Growth inhibition assay			Inhibition of human KS-1 cell growth in a cell viability assay, IC50=8.97341μM	SANGER
786-0	Growth inhibition assay			Inhibition of human 786-0 cell growth in a cell viability assay, IC50=8.99139μM	SANGER
SK-OV-3	Growth inhibition assay			Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.01236μM	SANGER
C3A	Growth inhibition assay			Inhibition of human C3A cell growth in a cell viability assay, IC50=9.12939μM	SANGER
NCI-H358	Growth inhibition assay			Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50=9.15929μM	SANGER
NCI-H2170	Growth inhibition assay			Inhibition of human NCI-H2170 cell growth in a cell viability assay, IC50=9.20801μM	SANGER
HMV-II	Growth inhibition assay			Inhibition of human HMV-II cell growth in a cell viability assay, IC50=9.34065μM	SANGER
SW1088	Growth inhibition assay			Inhibition of human SW1088 cell growth in a cell viability assay, IC50=9.56098μM	SANGER
RS4-11	Growth inhibition assay			Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=9.71841μM	SANGER
SNU-423	Growth inhibition assay			Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=9.87712μM	SANGER
A431	Growth inhibition assay			Inhibition of human A431 cell growth in a cell viability assay, IC50=9.88028μM	SANGER
BB65-RCC	Growth inhibition assay			Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=10.0298μM	SANGER
M059J	Growth inhibition assay			Inhibition of human M059J cell growth in a cell viability assay, IC50=10.2576μM	SANGER
Calu-3	Growth inhibition assay			Inhibition of human Calu-3 cell growth in a cell viability assay, IC50=10.5161μM	SANGER
LAMA-84	Growth inhibition assay			Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=10.6573μM	SANGER
ACHN	Growth inhibition assay			Inhibition of human ACHN cell growth in a cell viability assay, IC50=10.6743μM	SANGER
SW1990	Growth inhibition assay			Inhibition of human SW1990 cell growth in a cell viability assay, IC50=10.7009μM	SANGER
LC-2-ad	Growth inhibition assay			Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=10.7475μM	SANGER
U-698-M	Growth inhibition assay			Inhibition of human U-698-M cell growth in a cell viability assay, IC50=10.9926μM	SANGER
A2780	Growth inhibition assay			Inhibition of human A2780 cell growth in a cell viability assay, IC50=11.0963μM	SANGER
VA-ES-BJ	Growth inhibition assay			Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=11.1909μM	SANGER
A253	Growth inhibition assay			Inhibition of human A253 cell growth in a cell viability assay, IC50=11.3911μM	SANGER
NCI-H2087	Growth inhibition assay			Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=11.7288μM	SANGER
NTERA-S-cl-D1	Growth inhibition assay			Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=11.7718μM	SANGER
TE-12	Growth inhibition assay			Inhibition of human TE-12 cell growth in a cell viability assay, IC50=11.8178μM	SANGER
LNCaP-Clone-FGC	Growth inhibition assay			Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=12.358μM	SANGER
HT-1376	Growth inhibition assay			Inhibition of human HT-1376 cell growth in a cell viability assay, IC50=12.3595μM	SANGER
LB2518-MEL	Growth inhibition assay			Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=12.4325μM	SANGER
QIMR-WIL	Growth inhibition assay			Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=12.7363μM	SANGER
SF268	Growth inhibition assay			Inhibition of human SF268 cell growth in a cell viability assay, IC50=12.9423μM	SANGER
MES-SA	Growth inhibition assay			Inhibition of human MES-SA cell growth in a cell viability assay, IC50=13.2346μM	SANGER
BPH-1	Growth inhibition assay			Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=13.2694μM	SANGER
CA46	Growth inhibition assay			Inhibition of human CA46 cell growth in a cell viability assay, IC50=13.3899μM	SANGER
LB373-MEL-D	Growth inhibition assay			Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=13.4353μM	SANGER
NCI-H1755	Growth inhibition assay			Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=13.5203μM	SANGER
NCI-H1581	Growth inhibition assay			Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=13.742μM	SANGER
SNU-387	Growth inhibition assay			Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=13.9744μM	SANGER
HCC1419	Growth inhibition assay			Inhibition of human HCC1419 cell growth in a cell viability assay, IC50=14.1325μM	SANGER
TE-9	Growth inhibition assay			Inhibition of human TE-9 cell growth in a cell viability assay, IC50=14.5343μM	SANGER
LCLC-97TM1	Growth inhibition assay			Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=14.5912μM	SANGER
BC-1	Growth inhibition assay			Inhibition of human BC-1 cell growth in a cell viability assay, IC50=14.6038μM	SANGER
DU-145	Growth inhibition assay			Inhibition of human DU-145 cell growth in a cell viability assay, IC50=14.7605μM	SANGER
KARPAS-45	Growth inhibition assay			Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=15.1099μM	SANGER
SW684	Growth inhibition assay			Inhibition of human SW684 cell growth in a cell viability assay, IC50=15.1418μM	SANGER
HCC2218	Growth inhibition assay			Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=15.1714μM	SANGER
EW-13	Growth inhibition assay			Inhibition of human EW-13 cell growth in a cell viability assay, IC50=15.8055μM	SANGER
D-392MG	Growth inhibition assay			Inhibition of human D-392MG cell growth in a cell viability assay, IC50=15.8277μM	SANGER
PSN1	Growth inhibition assay			Inhibition of human PSN1 cell growth in a cell viability assay, IC50=15.8665μM	SANGER
Saos-2	Growth inhibition assay			Inhibition of human Saos-2 cell growth in a cell viability assay, IC50=15.9353μM	SANGER
COLO-679	Growth inhibition assay			Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=16.1233μM	SANGER
PC-14	Growth inhibition assay			Inhibition of human PC-14 cell growth in a cell viability assay, IC50=16.4902μM	SANGER
CAL-85-1	Growth inhibition assay			Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50=16.5837μM	SANGER
AU565	Growth inhibition assay			Inhibition of human AU565 cell growth in a cell viability assay, IC50=16.7598μM	SANGER
A2058	Growth inhibition assay			Inhibition of human A2058 cell growth in a cell viability assay, IC50=16.8504μM	SANGER
NH-12	Growth inhibition assay			Inhibition of human NH-12 cell growth in a cell viability assay, IC50=17.5557μM	SANGER
Hs-578-T	Growth inhibition assay			Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=17.6584μM	SANGER
RXF393	Growth inhibition assay			Inhibition of human RXF393 cell growth in a cell viability assay, IC50=17.8039μM	SANGER
COLO-741	Growth inhibition assay			Inhibition of human COLO-741 cell growth in a cell viability assay, IC50=18.1083μM	SANGER
NCI-H1355	Growth inhibition assay			Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=18.1318μM	SANGER
GI-ME-N	Growth inhibition assay			Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=18.453μM	SANGER
MEL-HO	Growth inhibition assay			Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=18.9753μM	SANGER
SW982	Growth inhibition assay			Inhibition of human SW982 cell growth in a cell viability assay, IC50=19.8406μM	SANGER
MONO-MAC-6	Growth inhibition assay			Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=19.9061μM	SANGER
MFH-ino	Growth inhibition assay			Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=20.2037μM	SANGER
BEN	Growth inhibition assay			Inhibition of human BEN cell growth in a cell viability assay, IC50=20.3128μM	SANGER
HT-144	Growth inhibition assay			Inhibition of human HT-144 cell growth in a cell viability assay, IC50=20.3697μM	SANGER
DoTc2-4510	Growth inhibition assay			Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50=20.7966μM	SANGER
NCI-H522	Growth inhibition assay			Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50=20.8971μM	SANGER
NCI-H1299	Growth inhibition assay			Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=21.167μM	SANGER
CAL-12T	Growth inhibition assay			Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=21.2435μM	SANGER
CTB-1	Growth inhibition assay			Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=21.6855μM	SANGER
COR-L105	Growth inhibition assay			Inhibition of human COR-L105 cell growth in a cell viability assay, IC50=21.7949μM	SANGER
NCI-H1650	Growth inhibition assay			Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50=21.8133μM	SANGER
SK-MEL-3	Growth inhibition assay			Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=21.9788μM	SANGER
697	Growth inhibition assay			Inhibition of human 697 cell growth in a cell viability assay, IC50=22.0402μM	SANGER
NEC8	Growth inhibition assay			Inhibition of human NEC8 cell growth in a cell viability assay, IC50=22.1998μM	SANGER
ACN	Growth inhibition assay			Inhibition of human ACN cell growth in a cell viability assay, IC50=22.4965μM	SANGER
MHH-PREB-1	Growth inhibition assay			Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=22.5088μM	SANGER
RPMI-6666	Growth inhibition assay			Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=22.5905μM	SANGER
BB30-HNC	Growth inhibition assay			Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=23.539μM	SANGER
HOS	Growth inhibition assay			Inhibition of human HOS cell growth in a cell viability assay, IC50=23.8014μM	SANGER
OVCAR-4	Growth inhibition assay			Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=23.984μM	SANGER
SK-HEP-1	Growth inhibition assay			Inhibition of human SK-HEP-1 cell growth in a cell viability assay, IC50=24.0791μM	SANGER
OS-RC-2	Growth inhibition assay			Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=24.0858μM	SANGER
MKN1	Growth inhibition assay			Inhibition of human MKN1 cell growth in a cell viability assay, IC50=24.1401μM	SANGER
NCI-H510A	Growth inhibition assay			Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=24.5517μM	SANGER
DBTRG-05MG	Growth inhibition assay			Inhibition of human DBTRG-05MG cell growth in a cell viability assay, IC50=25.014μM	SANGER
SW13	Growth inhibition assay			Inhibition of human SW13 cell growth in a cell viability assay, IC50=25.0254μM	SANGER
HuO-3N1	Growth inhibition assay			Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=25.2535μM	SANGER
U-2-OS	Growth inhibition assay			Inhibition of human U-2-OS cell growth in a cell viability assay, IC50=25.5982μM	SANGER
PANC-10-05	Growth inhibition assay			Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50=25.8389μM	SANGER
NUGC-3	Growth inhibition assay			Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50=26.0051μM	SANGER
MZ1-PC	Growth inhibition assay			Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=26.2821μM	SANGER
U-118-MG	Growth inhibition assay			Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=26.3272μM	SANGER
NCI-H1703	Growth inhibition assay			Inhibition of human NCI-H1703 cell growth in a cell viability assay, IC50=26.4593μM	SANGER
HT-1080	Growth inhibition assay			Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=26.6211μM	SANGER
EFO-21	Growth inhibition assay			Inhibition of human EFO-21 cell growth in a cell viability assay, IC50=26.7536μM	SANGER
TK10	Growth inhibition assay			Inhibition of human TK10 cell growth in a cell viability assay, IC50=27.1653μM	SANGER
ES1	Growth inhibition assay			Inhibition of human ES1 cell growth in a cell viability assay, IC50=27.6673μM	SANGER
DMS-153	Growth inhibition assay			Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=28.2498μM	SANGER
KYSE-270	Growth inhibition assay			Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=28.3533μM	SANGER
MLMA	Growth inhibition assay			Inhibition of human MLMA cell growth in a cell viability assay, IC50=28.3719μM	SANGER
KURAMOCHI	Growth inhibition assay			Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=28.5975μM	SANGER
NCI-H2347	Growth inhibition assay			Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50=28.5994μM	SANGER
MCF7	Growth inhibition assay			Inhibition of human MCF7 cell growth in a cell viability assay, IC50=28.7093μM	SANGER
HOP-92	Growth inhibition assay			Inhibition of human HOP-92 cell growth in a cell viability assay, IC50=28.9327μM	SANGER
REH	Growth inhibition assay			Inhibition of human REH cell growth in a cell viability assay, IC50=28.9422μM	SANGER
RT4	Growth inhibition assay			Inhibition of human RT4 cell growth in a cell viability assay, IC50=29.2259μM	SANGER
HT-1197	Growth inhibition assay			Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=29.2582μM	SANGER
BL-41	Growth inhibition assay			Inhibition of human BL-41 cell growth in a cell viability assay, IC50=29.6923μM	SANGER
IST-MES1	Growth inhibition assay			Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=29.8144μM	SANGER
MOLT-16	Growth inhibition assay			Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=30.3744μM	SANGER
GAK	Growth inhibition assay			Inhibition of human GAK cell growth in a cell viability assay, IC50=31.1007μM	SANGER
RD	Growth inhibition assay			Inhibition of human RD cell growth in a cell viability assay, IC50=31.2473μM	SANGER
COR-L23	Growth inhibition assay			Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=31.3023μM	SANGER
Capan-2	Growth inhibition assay			Inhibition of human Capan-2 cell growth in a cell viability assay, IC50=31.6669μM	SANGER
ALL-PO	Growth inhibition assay			Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=31.9592μM	SANGER
BCPAP	Growth inhibition assay			Inhibition of human BCPAP cell growth in a cell viability assay, IC50=32.4534μM	SANGER
OVCAR-3	Growth inhibition assay			Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=32.6497μM	SANGER
NKM-1	Growth inhibition assay			Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=33.1404μM	SANGER
647-V	Growth inhibition assay			Inhibition of human 647-V cell growth in a cell viability assay, IC50=33.9321μM	SANGER
ES5	Growth inhibition assay			Inhibition of human ES5 cell growth in a cell viability assay, IC50=34.9282μM	SANGER
A3-KAW	Growth inhibition assay			Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=35.5285μM	SANGER
ChaGo-K-1	Growth inhibition assay			Inhibition of human ChaGo-K-1 cell growth in a cell viability assay, IC50=35.5964μM	SANGER
NALM-6	Growth inhibition assay			Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=35.6045μM	SANGER
8-MG-BA	Growth inhibition assay			Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=35.9586μM	SANGER
BL-70	Growth inhibition assay			Inhibition of human BL-70 cell growth in a cell viability assay, IC50=36.8348μM	SANGER
MRK-nu-1	Growth inhibition assay			Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=37.0227μM	SANGER
COR-L88	Growth inhibition assay			Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=37.2976μM	SANGER
MDA-MB-415	Growth inhibition assay			Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=38.6783μM	SANGER
Becker	Growth inhibition assay			Inhibition of human Becker cell growth in a cell viability assay, IC50=39.1235μM	SANGER
NCI-H2452	Growth inhibition assay			Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=39.1445μM	SANGER
SW626	Growth inhibition assay			Inhibition of human SW626 cell growth in a cell viability assay, IC50=39.1841μM	SANGER
SAS	Growth inhibition assay			Inhibition of human SAS cell growth in a cell viability assay, IC50=39.5476μM	SANGER
DMS-53	Growth inhibition assay			Inhibition of human DMS-53 cell growth in a cell viability assay, IC50=39.7553μM	SANGER
CP66-MEL	Growth inhibition assay			Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=39.7602μM	SANGER
NCI-H2405	Growth inhibition assay			Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50=40.1926μM	SANGER
MC-CAR	Growth inhibition assay			Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=40.2471μM	SANGER
CAL-120	Growth inhibition assay			Inhibition of human CAL-120 cell growth in a cell viability assay, IC50=40.9723μM	SANGER
GCT	Growth inhibition assay			Inhibition of human GCT cell growth in a cell viability assay, IC50=41.2626μM	SANGER
A375	Growth inhibition assay			Inhibition of human A375 cell growth in a cell viability assay, IC50=41.5395μM	SANGER
MEG-01	Growth inhibition assay			Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=41.6116μM	SANGER
NCI-H2122	Growth inhibition assay			Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=41.97μM	SANGER
RPMI-2650	Growth inhibition assay			Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=43.4784μM	SANGER
8305C	Growth inhibition assay			Inhibition of human 8305C cell growth in a cell viability assay, IC50=43.7675μM	SANGER
NCI-H1395	Growth inhibition assay			Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=44.1055μM	SANGER
EW-16	Growth inhibition assay			Inhibition of human EW-16 cell growth in a cell viability assay, IC50=44.1094μM	SANGER
T98G	Growth inhibition assay			Inhibition of human T98G cell growth in a cell viability assay, IC50=44.4245μM	SANGER
IST-SL2	Growth inhibition assay			Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=44.9279μM	SANGER
NCI-H1651	Growth inhibition assay			Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=45.9208μM	SANGER
COR-L279	Growth inhibition assay			Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=46.2081μM	SANGER
YT	Growth inhibition assay			Inhibition of human YT cell growth in a cell viability assay, IC50=46.5067μM	SANGER
TE-11	Growth inhibition assay			Inhibition of human TE-11 cell growth in a cell viability assay, IC50=46.7404μM	SANGER
C-33-A	Growth inhibition assay			Inhibition of human C-33-A cell growth in a cell viability assay, IC50=46.8197μM	SANGER
OVCAR-5	Growth inhibition assay			Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50=47.2307μM	SANGER
PANC-03-27	Growth inhibition assay			Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=47.3513μM	SANGER
CaR-1	Growth inhibition assay			Inhibition of human CaR-1 cell growth in a cell viability assay, IC50=48.2474μM	SANGER
SNU-449	Growth inhibition assay			Inhibition of human SNU-449 cell growth in a cell viability assay, IC50=49.2285μM	SANGER
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (198.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.57mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.650mg/ml (3.77mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	437.52	Formula	C₂₁H₂₃N₇O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	444731-52-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GW786034			Smiles	CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N

Mechanism of Action

Targets/IC₅₀/Ki	VEGFR1 (Cell-free assay) 10 nM VEGFR2 (Cell-free assay) 30 nM VEGFR3 (Cell-free assay) 47 nM c-Kit (Cell-free assay) 74 nM PDGFR (Cell-free assay) 84 nM FGFR (Cell-free assay) 140 nM c-Fms (Cell-free assay) 146 nM
In vitro	Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. This compound shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1 µg/mL of this chemical and is completely abolished at 5 µg/mL. It induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in this compound-treated SYO-1 cells compared with that in the vehicle-treated cells. This chemical between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability.
Kinase Assay	Kinase enzyme assays
Kinase Assay	VEGFR enzyme assays for VEGGR1, VEGFR2, and VEGFR3 are run in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Reactions are initiated by the addition of 10 μL of activated VEGFR2 kinase solution [final concentration, 1 nM enzyme in 0.1 M HEPES, pH 7.5, containing 0.1 mg/mL bovine serum albumin (BSA), 300 μM dithiothreitol (DTT)] to 10 μL substrate solution [final concentration, 360 nM peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM ATP, 10 μM MgCl₂], and 1 μL of titrated this compound in DMSO. Plates are incubated at room temperature for 60 min, and then the reaction is quenched by the addition of 20 μL of 100 mM ethylene diamine tetraacetic acid (EDTA). After quenching, 20 μL HTRF reagents (final concentration, 15 nM Streptavidin-linked allophycocyanin, 1 nM Europium-labeled antiphosphotyrosine antibody diluted in 0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5) is added and the plates incubated for a minimum of 10 min. The fluorescence at 665 nM is measured with a Wallac Victor plate reader using a time delay of 50 μs.
In vivo	The mice treated with 30 mg/kg or 100 mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10 mg/kg this compound. Treatment with this agent is well-tolerated and there is no significant difference in the body weight among the mice in each group.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18620382/ [2] https://pubmed.ncbi.nlm.nih.gov/22359392/ [3] https://pubmed.ncbi.nlm.nih.gov/22466477/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p53 / PUMA p-Akt / Akt		27924057
Growth inhibition assay	Cell viability		27924057

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03850964	Recruiting	Hereditary Hemorrhagic Telangiectasia\|Epistaxis\|Anemia\|Nosebleed\|HHT	Cure HHT	May 8 2023	Phase 2\|Phase 3
NCT05180695	Recruiting	Advanced Soft-tissue Sarcoma\|Metastatic Soft-tissue Sarcoma	Centre Leon Berard\|Novartis\|National Cancer Institute France	April 15 2022	Phase 1\|Phase 2
NCT03735758	Terminated	Soft Tissue Sarcoma Adult	GWT-TUD GmbH	November 2 2018	Phase 4

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