- 阻害剤
- 研究分野別
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- 化合物ライブラリー
- 抗体
- 新製品
- お問い合わせ
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.
CAS No. 444731-52-6
文献中Selleckの製品使用例（78）
製品安全説明書
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純度：
99.95%
99.95
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 |
|
| 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 |
| 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 |
DMSO : 88 mg/mL ( (201.13 mM)； 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 Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
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
匹
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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他に質問がある場合は、お気軽にお問い合わせください。
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