Pazopanib

別名:GW786034

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. Pazopanib induces cathepsin B activation and autophagy.

Pazopanib化学構造

CAS No. 444731-52-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 16300 国内在庫あり
JPY 13600 国内在庫あり
JPY 36800 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(73)

製品安全説明書

現在のバッチを見る: 純度: 99.98%
99.98

Pazopanib関連製品

シグナル伝達経路

VEGFR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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 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
RT-112 Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.10376μM SANGER
CCF-STTG1 Growth inhibition assay Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.04981μM SANGER
MG-63 Growth inhibition assay Inhibition of human MG-63 cell growth in a cell viability assay, IC50=1.00146μM SANGER
HT55 Growth inhibition assay Inhibition of human HT55 cell growth in a cell viability assay, IC50=0.98781μM SANGER
KG-1 Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=0.71755μM SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.65987μM SANGER
MFE-296 Growth inhibition assay Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=0.59022μM SANGER
G-402 Growth inhibition assay Inhibition of human G-402 cell growth in a cell viability assay, IC50=0.53184μM SANGER
A204 Growth inhibition assay Inhibition of human A204 cell growth in a cell viability assay, IC50=0.10906μM SANGER
GDM-1 Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.10399μM SANGER
CGTH-W-1 Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=0.04001μM SANGER
AN3-CA Growth inhibition assay Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=0.01005μM SANGER
EoL-1-cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000289μM SANGER
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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
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
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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
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
human HN5 cells Proliferation assay Antiproliferative activity against human HN5 cells in serum containing medium 18620382
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
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 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. Pazopanib induces cathepsin B activation and autophagy.
Targets
VEGFR1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
PDGFR [1]
(Cell-free assay)
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10 nM 30 nM 47 nM 74 nM 84 nM
In Vitro
In vitro

Pazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. [1]

PPazopanib 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 Pazopanib and is completely abolished at 5 µg/mL. Pazopanib 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 Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. [2]

Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability. [3]

Kinase Assay Kinase enzyme assays
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 Pazopanib 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p53 / PUMA p-Akt / Akt 27924057
Growth inhibition assay Cell viability 27924057
In Vivo
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 Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group. [2]

動物実験 動物モデル Immunodeficient mice bearing SYO-1 cells
投与量 0 mg/kg, 10 mg/kg, 30 mg/kg, or 100 mg/kg
投与経路 Oral administration
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
NCT04659343 Unknown status
Kidney Cancer|Renal Cell Carcinoma Metastatic|Drug Toxicity|Drug Side Effect|Drug Mechanism
Frede Donskov|Odense University Hospital|Herlev Hospital|Rigshospitalet Denmark|University of Aarhus
November 1 2020 --
NCT03735758 Terminated
Soft Tissue Sarcoma Adult
GWT-TUD GmbH
November 2 2018 Phase 4

化学情報

分子量 437.52 化学式

C21H23N7O2S

CAS No. 444731-52-6 SDF Download Pazopanib SDFをダウンロードする
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
保管

In vitro
Batch:

DMSO : 87 mg/mL ( (198.84 mM); Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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