Pazopanib HCl
别名: GW786034 HCl 中文名称：盐酸帕佐帕尼
Pazopanib HCl是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。
Pazopanib HCl Chemical Structure
CAS: 635702-64-6
产品质控
批次：
纯度：
99.93%
99.93
Pazopanib HCl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 |
| INA-6 | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| Dox40 | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| RPMI | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| MM.1R | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| MM.1S | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| OPM2 | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| U266 | Growth inhibitory assay | 10 μg/mL | inhibits MM Cell Growth | 17164332 | |
| MM.1S | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| MM.1R | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| RPMI | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| Dox40 | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| INA-6 | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| OPM2 | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| U266 | cytotoxicity assay | 20 μg/mL | inhibits MM Cell Survival | 17164332 | |
| HBMEC | Growth inhibitory assay | ~10 μM | IC50=1 μM | 21081656 | |
| HBMEC | Function assay | ~1 μM | abrogates the phosphorylation of VEGFR2 with disruption of downstream PLCγ1 | 21081656 | |
| HBMEC | Function assay | ~1 μM | disrupts the Ras-Raf-ERK pathway through decreased phosphorylated MEK1/2 and ERK1/2 | 21081656 | |
| HBMEC | Function assay | ~20 μM | disrupts 50% of tube formation at 1 μM | 21081656 | |
| MDA-MB-231 | Growth inhibitory assay | ~10 μM | IC50=5 μM | 21081656 | |
| MDA-MB-231 | Function assay | 0.5 μM | inhibits the ERK1/2 signaling pathway | 21081656 | |
| MDA-MB-231 | Function assay | 5 μM | induces a cell-cycle arrest | 21081656 | |
| J82 | cytotoxicity assay | ~10 μM | IC50=24.57 μM | 21529900 | |
| T24 | cytotoxicity assay | ~10 μM | IC50=52.45 μM | 21529900 | |
| HT1376 | cytotoxicity assay | ~10 μM | IC50=28.21 μM | 21529900 | |
| RT4 | cytotoxicity assay | ~10 μM | IC50=5.14 μM | 21529900 | |
| CRL1749 | cytotoxicity assay | ~10 μM | IC50=22.69 μM | 21529900 | |
| HTB9 | cytotoxicity assay | ~10 μM | IC50=11.84 μM | 21529900 | |
| Sup | cytotoxicity assay | ~10 μM | IC50=53.32 μM | 21529900 | |
| HTB3 | cytotoxicity assay | ~10 μM | IC50=14.16 μM | 21529900 | |
| CEC | Function assay | ~10 μg/mL | down-regulates VEGF levels | 21620822 | |
| RPE | Function assay | ~10 μg/mL | down-regulates VEGF levels | 21620822 | |
| CEC | Function assay | ~5 μg/mL | blocks endothelial cell migration | 21620822 | |
| 5637 | Autophagy assay | 20 μM | triggers the autophagic process | 23887605 | |
| J82 | Autophagy assay | 20 μM | triggers the autophagic process | 23887605 | |
| 5637 | Function assay | 20 μM | induces lysosomal-dependent necrosis | 23887605 | |
| J82 | Function assay | 20 μM | induces lysosomal-dependent necrosis | 23887605 | |
| 5637 | Function assay | 20 μM | induces lysosome alteration and inhibits CB activity | 23887605 | |
| J82 | Function assay | 20 μM | induces lysosome alteration and inhibits CB activity | 23887605 | |
| KATO-II | Growth inhibitory assay | 5 μM | blocks proliferation | 25249557 | |
| OCUM-2M | Growth inhibitory assay | 5 μM | blocks proliferation | 25249557 | |
| SNU-16 | Growth inhibitory assay | 5 μM | blocks proliferation | 25249557 | |
| HSC-39 | Growth inhibitory assay | 5 μM | blocks proliferation | 25249557 | |
| KATO-II | cytotoxicity assay | ~10 μM | IC50=0.1 to 2.0 μmol/L | 25249557 | |
| OCUM-2M | cytotoxicity assay | ~10 μM | IC50=0.1 to 2.0 μmol/L | 25249557 | |
| SNU-16 | cytotoxicity assay | ~10 μM | IC50=0.1 to 2.0 μmol/L | 25249557 | |
| HSC-39 | cytotoxicity assay | ~10 μM | IC50=0.1 to 2.0 μmol/L | 25249557 | |
| NIH 3T3 | Growth inhibitory assay | ~10 μM | inhibits cell growth and colony formation | 25249557 | |
| KATO-III | Function assay | 1 μM | induces cell-cycle arrest | 25249557 | |
| OCUM-2M | Function assay | 1 μM | induces cell-cycle arrest | 25249557 | |
| KATO-III | Apoptosis assay | 1 μM | induces apoptosis | 25249557 | |
| OCUM-2M | Apoptosis assay | 1 μM | induces apoptosis | 25249557 | |
| KATO-III | Function assay | 1 μM | inhibits FGFR2 phosphorylation and downstream signaling molecules | 25249557 | |
| 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 | |
| MM | Kinase assay | inhibits VEGF-induced phosphorylation of flt1 | 17164332 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A375P | Antiproliferative assay | Antiproliferative activity against human A375P cells in serum containing medium | 18620382 | ||
| HN5 | Antiproliferative assay | Antiproliferative activity against human HN5 cells in serum containing medium | 18620382 | ||
| HT29 | Antiproliferative assay | Antiproliferative activity against human HT29 cells in serum containing medium | 18620382 | ||
| MM.1S | Function assay | suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. | 17164332 | ||
| MM.1R | Function assay | suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. | 17164332 | ||
| Dox40 | Function assay | suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. | 17164332 | ||
| OPM2 | Function assay | suppresses VEGF-Induced Endothelial Cell Proliferation and Migration. | 17164332 | ||
| 5637 | Growth inhibitory assay | IC50=15.0 μM | 23887605 | ||
| J82 | Growth inhibitory assay | IC50=18.4 μM | 23887605 | ||
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Pazopanib HCl是一种新型多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR，FGFR，c-Kit和c-fms，在无细胞试验中IC50分别是10 nM，30 nM，47 nM，84 nM，74 nM，140 nM和146 nM。Pazopanib 可诱导自噬II型细胞死亡。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | Pazopanib是一个多激酶的抑制剂。 | |||||||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在HUVEC细胞中，Pazopanib显著抑制VEGF诱导的VEGFR-2的磷酸化，IC50 为8nM [1]。 在所有滑膜肉瘤细胞系中Pazopanib都表现出了生长抑制作用，包括SYO-1和HS-SY-II细胞，这种抑制具有剂量依赖的特性。1µg/mL Pazopanib就可以抑制SYO-1和HS-SY-II细胞增殖，而5µg/mL Pazopanib可以让它们的增殖彻底受阻。 Pazopanib 会诱导滑膜肉瘤细胞周期停留在 G1期从而抑制它的生长。与对照的细胞相比，经过Pazopanib处理过的 SYO-1细胞中的AKTs, GSK-3β, JNKs, p70 S6激酶以及mTOR的磷酸化都受到了抑制[2]。在20 mg/mL 到 22.5 mg/mL的浓度之间，Pazopanib 使RPE细胞的生存能力逐渐下降[3]。 | |||
|---|---|---|---|---|
| 激酶实验 | 激酶活性测定 | |||
| 通过杆状病毒表达系统纯化人源的VEGFR受体激酶1, 2和3的C端催化活性区域的GST融合蛋白，用这些蛋白在384孔微量滴定板上利用均相时间分辨荧光技术(HTRF)对VEGRF1,2和3的酶活性进行分析。首先将10 μL活化的VEGFR2激酶溶液[终浓度为1nM酶溶于0.1 M HEPES，pH 7.5,包含0.1 mg/mL BSA，300 μM DTT]加入10μL底物溶液[终浓度为360 nM多肽（生物素偶联的aminohexyl-EEEEYFELVAKKKK-NH2），75 μM ATP, 10 μM MgCl2]，同时加入1 μL 溶解在DMSO中的Pazopanib。滴定板在室温条件下孵育1小时，然后加入20 μL 100 mM 的EDTA终止反应。终止之后，加入20μL HTRF试剂（终浓度为15 nM 链亲和素偶联的别藻蓝素，用0.1 mg/mL BSA, 0.1 M HEPES, pH 7.5稀释的1 nM铕标记的酪氨酸磷酸化抗体）孵育十分钟以上。使用Wallac Victor的时间分辨荧光仪测定665 nM处的荧光值，时间间隔为50 μs。 | ||||
| 细胞实验 | 细胞系 | HUVEC细胞 | ||
| 浓度 | 0 μM -10 μM | |||
| 孵育时间 | 1 小时 | |||
| 方法 | 检测经过VEGF处理过的HUVEC细胞中VEGFR2的磷酸化水平。细胞按每板100万到150万个的密度培养在铺有I型胶原蛋白的10 cm平板上，培养基选用 Clonetics EGM-MV。培养24小时后, 将原来的培养基换成含有0.1% BSA和500 μg/mL hydrocortisone 的Clonetics EBM 培养基，对细胞进行过夜的血清饥饿处理。然后用不同浓度的 Pazopanib 处理细胞1小时, 随后用10 ng/mL 的VEGF 或者对照物处理细胞10分钟。将细胞溶解在裂解液中。用flk-1的抗体对VEGFR2进行免疫沉淀反应，随后进行SDS-聚丙烯酰胺凝胶电泳，然后用flk-1 或者 antiphosphotyrosine (anti-P-tyr-biotin)的抗体进行蛋白免疫印迹的检测。通过光密度法测量将VEGFR2的磷酸化水平量化并将总的VEGFR2水品标准化。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p53 / PUMA p-Akt / Akt p-VEGFR2 / p-c-Kit / p-PDGFRβ / FLT-3 |
|
27924057 | |
| Immunofluorescence | YAP/TAZ |
|
26199863 | |
| Growth inhibition assay | Cell viability |
|
27924057 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 与没有经过Pazopanib或者仅用10 mg/kg的Pazopanib治疗的小鼠相比，经过30 mg/kg或者100 mg/kg Pazopanib治疗的小鼠其肿瘤症状明显减轻。Pazopanib治疗耐受性良好，各组小鼠之间体重没有发生明显差异[2]。 | |
|---|---|---|
| 动物实验 | Animal Models | 携带SYO-1细胞的免疫缺陷小鼠 |
| Dosages | 0 mg/kg, 10 mg/kg, 30 mg/kg或100 mg/kg | |
| Administration | 口服 | |
| 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 |
化学信息&溶解度
| 分子量 | 473.98 | 分子式 | C21H23N7O2S.HCl |
| CAS号 | 635702-64-6 | SDF | Download Pazopanib HCl 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.Cl | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 17 mg/mL ( (35.86 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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