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別名: GW786034 中文名稱:帕唑帕尼
Pazopanib (GW786034) 是一種新型多靶點的VEGFR1,VEGFR2,VEGFR3,PDGFR,F(xiàn)GFR,c-Kit 和 c-Fms/CSF1R抑制劑,無細胞試驗中IC50分別為10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。Pazopanib 可誘導(dǎo) cathepsin B 的活化和自噬。
Pazopanib Chemical Structure
CAS: 444731-52-6
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
---|---|---|---|---|---|
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 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Pazopanib (GW786034) 是一種新型多靶點的VEGFR1,VEGFR2,VEGFR3,PDGFR,F(xiàn)GFR,c-Kit 和 c-Fms/CSF1R抑制劑,無細胞試驗中IC50分別為10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。Pazopanib 可誘導(dǎo) cathepsin B 的活化和自噬。 | |||||||||||
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Pazopanib有效抑制VEGF誘導(dǎo)的HUVEC 細胞中VEGFR2磷酸化作用,IC50為8 nM。[1] 在所有滑膜肉瘤細胞系,包括SYO-1和HS-SY-II細胞中,Pazopanib表現(xiàn)出劑量依賴性生長抑制作用。SYO-1和HS-SY-II細胞的增殖在1微克/毫升的Pazopanib下被抑制,在5微克/毫升的Pazopanib下被完全廢止。Pazopanib引起G1期阻滯,并且因此抑制滑膜肉瘤細胞的生長。與載體處理的細胞相比,Akts,GSK-3β,JNKs,p70 S6 激酶,和mTOR的磷酸化作用在Pazopanib處理的SYO-1細胞中被抑制。[2] Pazopanib在20毫克/毫升和22.5毫克/毫升之間表現(xiàn)出逐漸增加的RPE細胞活性降低。[3] |
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實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
Western blot | p-Akt / Akt p53 / PUMA |
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27924057 | |
Growth inhibition assay | Cell viability |
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27924057 |
體內(nèi)研究(In Vivo) | ||
體內(nèi)研究活性 | 與用載體或10毫克/千克Pazopanib處理的小鼠相比,用30毫克/千克或100毫克/千克Pazopanib處理的小鼠,腫瘤負荷顯著降低。Pazopanib治療具有良好的耐受性,并且每組小鼠的體重差異沒有明顯不同。[2] |
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動物實驗 | Animal Models | 含有SYO-1細胞的免疫缺陷小鼠 |
Dosages | 0 毫克/千克, 10 毫克/千克, 30毫克/千克, 或100?毫克/千克 | |
Administration | 口服給藥 |
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 |
分子量 | 437.52 | 分子式 | C21H23N7O2S |
CAS號 | 444731-52-6 | SDF | Download Pazopanib SDF |
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 | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 88 mg/mL ( (201.13 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
體內(nèi)溶解度 現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 |
動物體內(nèi)配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)
計算結(jié)果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);
體內(nèi)配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內(nèi)配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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