pour la recherche uniquement
Pazopanib VEGFR inhibiteur
Réf. CatalogueS3012
Structure chimique
Poids moléculaire: 437.52
Aller à
Contrôle Qualité
Lot :
Pureté :
99.98%
99.98
| Cibles apparentées | EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit |
|---|---|
| Autre VEGFR Inhibiteurs | SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl |
Culture cellulaire, traitement et concentration de travail
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | PMID |
|---|---|---|---|---|---|---|
| human HT29 cells | Proliferation assay | Antiproliferative activity against human HT29 cells in serum containing medium | 18620382 | |||
| human A375P cells | Proliferation assay | Antiproliferative activity against human A375P cells in serum containing medium | 18620382 | |||
| human HN5 cells | Proliferation assay | Antiproliferative activity against human HN5 cells in serum containing medium | 18620382 | |||
| HUVEC | Function assay | 1 μM | 6 h | Antiangiogenic activity in HUVEC assessed as inhibition of tube formation at 0.1 uM after 6 hrs by Matrigel assay | 24036042 | |
| HT-29 | Function assay | 14 to 24 hrs | Inhibition of RIPK1 in human HT-29 cells assessed as reduction in TNFalpha-induced necroptosis incubated for 14 to 24 hrs in presence of Smac mimetic and z-VAD-FMK by cell titer glo-based luminescence assay, IC50=0.873μM | 31622096 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | |||
| HUVEC | Function assay | 100 nM | 2 hrs | Inhibition of VEGF-stimulated VEGFR2 phosphorylation in human HUVEC cells at 100 nM preincubated for 2 hrs followed by VEGF stimulation by Western blot analysis | 29787262 | |
| HUVEC | Antiangiogenic assay | 0.1 uM | 6 hrs | Antiangiogenic activity in human HUVEC cells assessed as reduction in capillary-like tubular network formation at 0.1 uM after 6 hrs by phase-contrast microscopy | 29787262 | |
| EoL-1-cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=0.0000289μM | SANGER | |||
| AN3-CA | Growth inhibition assay | Inhibition of human AN3-CA cell growth in a cell viability assay, IC50=0.01005μM | SANGER | |||
| CGTH-W-1 | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=0.04001μM | SANGER | |||
| GDM-1 | Growth inhibition assay | Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.10399μM | SANGER | |||
| A204 | Growth inhibition assay | Inhibition of human A204 cell growth in a cell viability assay, IC50=0.10906μM | SANGER | |||
| G-402 | Growth inhibition assay | Inhibition of human G-402 cell growth in a cell viability assay, IC50=0.53184μM | SANGER | |||
| MFE-296 | Growth inhibition assay | Inhibition of human MFE-296 cell growth in a cell viability assay, IC50=0.59022μM | SANGER | |||
| NOS-1 | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.65987μM | SANGER | |||
| KG-1 | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay, IC50=0.71755μM | SANGER | |||
| HT55 | Growth inhibition assay | Inhibition of human HT55 cell growth in a cell viability assay, IC50=0.98781μM | SANGER | |||
| MG-63 | Growth inhibition assay | Inhibition of human MG-63 cell growth in a cell viability assay, IC50=1.00146μM | SANGER | |||
| CCF-STTG1 | Growth inhibition assay | Inhibition of human CCF-STTG1 cell growth in a cell viability assay, IC50=1.04981μM | SANGER | |||
| RT-112 | Growth inhibition assay | Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.10376μM | SANGER | |||
| MC-IXC | Growth inhibition assay | Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=1.11512μM | SANGER | |||
| HUTU-80 | Growth inhibition assay | Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.28103μM | SANGER | |||
| MV-4-11 | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=1.34501μM | SANGER | |||
| LCLC-103H | Growth inhibition assay | Inhibition of human LCLC-103H cell growth in a cell viability assay, IC50=1.44549μM | SANGER | |||
| G-401 | Growth inhibition assay | Inhibition of human G-401 cell growth in a cell viability assay, IC50=1.46421μM | SANGER | |||
| A704 | Growth inhibition assay | Inhibition of human A704 cell growth in a cell viability assay, IC50=1.60323μM | SANGER | |||
| ESS-1 | Growth inhibition assay | Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=1.60396μM | SANGER | |||
| HLE | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=1.63804μM | SANGER | |||
| NY | Growth inhibition assay | Inhibition of human NY cell growth in a cell viability assay, IC50=1.84821μM | SANGER | |||
| A427 | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50=1.98075μM | SANGER | |||
| SK-N-DZ | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=2.02381μM | SANGER | |||
| J82 | Growth inhibition assay | Inhibition of human J82 cell growth in a cell viability assay, IC50=2.06088μM | SANGER | |||
| GI-1 | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay, IC50=2.22951μM | SANGER | |||
| NCI-H716 | Growth inhibition assay | Inhibition of human NCI-H716 cell growth in a cell viability assay, IC50=2.31633μM | SANGER | |||
| SF126 | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50=2.47459μM | SANGER | |||
| H4 | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50=2.51262μM | SANGER | |||
| LB831-BLC | Growth inhibition assay | Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=2.54566μM | SANGER | |||
| HCC1395 | Growth inhibition assay | Inhibition of human HCC1395 cell growth in a cell viability assay, IC50=2.58156μM | SANGER | |||
| LK-2 | Growth inhibition assay | Inhibition of human LK-2 cell growth in a cell viability assay, IC50=2.64569μM | SANGER | |||
| G-361 | Growth inhibition assay | Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.04082μM | SANGER | |||
| NCI-H2342 | Growth inhibition assay | Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=3.13316μM | SANGER | |||
| SK-LU-1 | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.18767μM | SANGER | |||
| IGROV-1 | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=3.24713μM | SANGER | |||
| EB2 | Growth inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50=3.28168μM | SANGER | |||
| CAL-54 | Growth inhibition assay | Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=3.28367μM | SANGER | |||
| OCUB-M | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=3.31368μM | SANGER | |||
| LB1047-RCC | Growth inhibition assay | Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=3.53164μM | SANGER | |||
| Daudi | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=3.66219μM | SANGER | |||
| A172 | Growth inhibition assay | Inhibition of human A172 cell growth in a cell viability assay, IC50=3.7379μM | SANGER | |||
| KGN | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay, IC50=4.06709μM | SANGER | |||
| SNG-M | Growth inhibition assay | Inhibition of human SNG-M cell growth in a cell viability assay, IC50=4.08669μM | SANGER | |||
| SW1710 | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=4.47318μM | SANGER | |||
| Daoy | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50=4.77949μM | SANGER | |||
| DMS-273 | Growth inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50=4.96202μM | SANGER | |||
| KU812 | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=5.37812μM | SANGER | |||
| NCI-H727 | Growth inhibition assay | Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50=5.40901μM | SANGER | |||
| P30-OHK | Growth inhibition assay | Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=5.4694μM | SANGER | |||
| MIA-PaCa-2 | Growth inhibition assay | Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50=5.60466μM | SANGER | |||
| TT | Growth inhibition assay | Inhibition of human TT cell growth in a cell viability assay, IC50=5.6624μM | SANGER | |||
| DK-MG | Growth inhibition assay | Inhibition of human DK-MG cell growth in a cell viability assay, IC50=5.72028μM | SANGER | |||
| GB-1 | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=5.73434μM | SANGER | |||
| NCI-H520 | Growth inhibition assay | Inhibition of human NCI-H520 cell growth in a cell viability assay, IC50=5.73435μM | SANGER | |||
| WM-115 | Growth inhibition assay | Inhibition of human WM-115 cell growth in a cell viability assay, IC50=5.75644μM | SANGER | |||
| CAL-72 | Growth inhibition assay | Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=5.9381μM | SANGER | |||
| NCI-H1573 | Growth inhibition assay | Inhibition of human NCI-H1573 cell growth in a cell viability assay, IC50=5.96542μM | SANGER | |||
| ES6 | Growth inhibition assay | Inhibition of human ES6 cell growth in a cell viability assay, IC50=6.02688μM | SANGER | |||
| TE-8 | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50=6.16473μM | SANGER | |||
| GAMG | Growth inhibition assay | Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.17776μM | SANGER | |||
| HGC-27 | Growth inhibition assay | Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=6.2015μM | SANGER | |||
| CTV-1 | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=6.20903μM | SANGER | |||
| NCI-H810 | Growth inhibition assay | Inhibition of human NCI-H810 cell growth in a cell viability assay, IC50=6.31365μM | SANGER | |||
| NMC-G1 | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=6.55237μM | SANGER | |||
| SNB75 | Growth inhibition assay | Inhibition of human SNB75 cell growth in a cell viability assay, IC50=6.56939μM | SANGER | |||
| SK-MES-1 | Growth inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50=6.8663μM | SANGER | |||
| MZ2-MEL | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=6.93016μM | SANGER | |||
| TE-15 | Growth inhibition assay | Inhibition of human TE-15 cell growth in a cell viability assay, IC50=7.16924μM | SANGER | |||
| S-117 | Growth inhibition assay | Inhibition of human S-117 cell growth in a cell viability assay, IC50=7.57924μM | SANGER | |||
| HuH-7 | Growth inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=7.69384μM | SANGER | |||
| CAS-1 | Growth inhibition assay | Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=7.76339μM | SANGER | |||
| D-502MG | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay, IC50=7.78222μM | SANGER | |||
| IA-LM | Growth inhibition assay | Inhibition of human IA-LM cell growth in a cell viability assay, IC50=7.93364μM | SANGER | |||
| CAKI-1 | Growth inhibition assay | Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=8.28831μM | SANGER | |||
| KYSE-70 | Growth inhibition assay | Inhibition of human KYSE-70 cell growth in a cell viability assay, IC50=8.45447μM | SANGER | |||
| HCC1569 | Growth inhibition assay | Inhibition of human HCC1569 cell growth in a cell viability assay, IC50=8.46556μM | SANGER | |||
| SR | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay, IC50=8.70202μM | SANGER | |||
| SH-4 | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay, IC50=8.73653μM | SANGER | |||
| SW954 | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50=8.75347μM | SANGER | |||
| MPP-89 | Growth inhibition assay | Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=8.7782μM | SANGER | |||
| IST-MEL1 | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=8.91086μM | SANGER | |||
| EFM-19 | Growth inhibition assay | Inhibition of human EFM-19 cell growth in a cell viability assay, IC50=8.92276μM | SANGER | |||
| KS-1 | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=8.97341μM | SANGER | |||
| 786-0 | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=8.99139μM | SANGER | |||
| SK-OV-3 | Growth inhibition assay | Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.01236μM | SANGER | |||
| C3A | Growth inhibition assay | Inhibition of human C3A cell growth in a cell viability assay, IC50=9.12939μM | SANGER | |||
| NCI-H358 | Growth inhibition assay | Inhibition of human NCI-H358 cell growth in a cell viability assay, IC50=9.15929μM | SANGER | |||
| NCI-H2170 | Growth inhibition assay | Inhibition of human NCI-H2170 cell growth in a cell viability assay, IC50=9.20801μM | SANGER | |||
| HMV-II | Growth inhibition assay | Inhibition of human HMV-II cell growth in a cell viability assay, IC50=9.34065μM | SANGER | |||
| SW1088 | Growth inhibition assay | Inhibition of human SW1088 cell growth in a cell viability assay, IC50=9.56098μM | SANGER | |||
| RS4-11 | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=9.71841μM | SANGER | |||
| SNU-423 | Growth inhibition assay | Inhibition of human SNU-423 cell growth in a cell viability assay, IC50=9.87712μM | SANGER | |||
| A431 | Growth inhibition assay | Inhibition of human A431 cell growth in a cell viability assay, IC50=9.88028μM | SANGER | |||
| BB65-RCC | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=10.0298μM | SANGER | |||
| M059J | Growth inhibition assay | Inhibition of human M059J cell growth in a cell viability assay, IC50=10.2576μM | SANGER | |||
| Calu-3 | Growth inhibition assay | Inhibition of human Calu-3 cell growth in a cell viability assay, IC50=10.5161μM | SANGER | |||
| LAMA-84 | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=10.6573μM | SANGER | |||
| ACHN | Growth inhibition assay | Inhibition of human ACHN cell growth in a cell viability assay, IC50=10.6743μM | SANGER | |||
| SW1990 | Growth inhibition assay | Inhibition of human SW1990 cell growth in a cell viability assay, IC50=10.7009μM | SANGER | |||
| LC-2-ad | Growth inhibition assay | Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=10.7475μM | SANGER | |||
| U-698-M | Growth inhibition assay | Inhibition of human U-698-M cell growth in a cell viability assay, IC50=10.9926μM | SANGER | |||
| A2780 | Growth inhibition assay | Inhibition of human A2780 cell growth in a cell viability assay, IC50=11.0963μM | SANGER | |||
| VA-ES-BJ | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=11.1909μM | SANGER | |||
| A253 | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay, IC50=11.3911μM | SANGER | |||
| NCI-H2087 | Growth inhibition assay | Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=11.7288μM | SANGER | |||
| NTERA-S-cl-D1 | Growth inhibition assay | Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=11.7718μM | SANGER | |||
| TE-12 | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50=11.8178μM | SANGER | |||
| LNCaP-Clone-FGC | Growth inhibition assay | Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=12.358μM | SANGER | |||
| HT-1376 | Growth inhibition assay | Inhibition of human HT-1376 cell growth in a cell viability assay, IC50=12.3595μM | SANGER | |||
| LB2518-MEL | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=12.4325μM | SANGER | |||
| QIMR-WIL | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=12.7363μM | SANGER | |||
| SF268 | Growth inhibition assay | Inhibition of human SF268 cell growth in a cell viability assay, IC50=12.9423μM | SANGER | |||
| MES-SA | Growth inhibition assay | Inhibition of human MES-SA cell growth in a cell viability assay, IC50=13.2346μM | SANGER | |||
| BPH-1 | Growth inhibition assay | Inhibition of human BPH-1 cell growth in a cell viability assay, IC50=13.2694μM | SANGER | |||
| CA46 | Growth inhibition assay | Inhibition of human CA46 cell growth in a cell viability assay, IC50=13.3899μM | SANGER | |||
| LB373-MEL-D | Growth inhibition assay | Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=13.4353μM | SANGER | |||
| NCI-H1755 | Growth inhibition assay | Inhibition of human NCI-H1755 cell growth in a cell viability assay, IC50=13.5203μM | SANGER | |||
| NCI-H1581 | Growth inhibition assay | Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=13.742μM | SANGER | |||
| SNU-387 | Growth inhibition assay | Inhibition of human SNU-387 cell growth in a cell viability assay, IC50=13.9744μM | SANGER | |||
| HCC1419 | Growth inhibition assay | Inhibition of human HCC1419 cell growth in a cell viability assay, IC50=14.1325μM | SANGER | |||
| TE-9 | Growth inhibition assay | Inhibition of human TE-9 cell growth in a cell viability assay, IC50=14.5343μM | SANGER | |||
| LCLC-97TM1 | Growth inhibition assay | Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=14.5912μM | SANGER | |||
| BC-1 | Growth inhibition assay | Inhibition of human BC-1 cell growth in a cell viability assay, IC50=14.6038μM | SANGER | |||
| DU-145 | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=14.7605μM | SANGER | |||
| KARPAS-45 | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=15.1099μM | SANGER | |||
| SW684 | Growth inhibition assay | Inhibition of human SW684 cell growth in a cell viability assay, IC50=15.1418μM | SANGER | |||
| HCC2218 | Growth inhibition assay | Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=15.1714μM | SANGER | |||
| EW-13 | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=15.8055μM | SANGER | |||
| D-392MG | Growth inhibition assay | Inhibition of human D-392MG cell growth in a cell viability assay, IC50=15.8277μM | SANGER | |||
| PSN1 | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50=15.8665μM | SANGER | |||
| Saos-2 | Growth inhibition assay | Inhibition of human Saos-2 cell growth in a cell viability assay, IC50=15.9353μM | SANGER | |||
| COLO-679 | Growth inhibition assay | Inhibition of human COLO-679 cell growth in a cell viability assay, IC50=16.1233μM | SANGER | |||
| PC-14 | Growth inhibition assay | Inhibition of human PC-14 cell growth in a cell viability assay, IC50=16.4902μM | SANGER | |||
| CAL-85-1 | Growth inhibition assay | Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50=16.5837μM | SANGER | |||
| AU565 | Growth inhibition assay | Inhibition of human AU565 cell growth in a cell viability assay, IC50=16.7598μM | SANGER | |||
| A2058 | Growth inhibition assay | Inhibition of human A2058 cell growth in a cell viability assay, IC50=16.8504μM | SANGER | |||
| NH-12 | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=17.5557μM | SANGER | |||
| Hs-578-T | Growth inhibition assay | Inhibition of human Hs-578-T cell growth in a cell viability assay, IC50=17.6584μM | SANGER | |||
| RXF393 | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay, IC50=17.8039μM | SANGER | |||
| COLO-741 | Growth inhibition assay | Inhibition of human COLO-741 cell growth in a cell viability assay, IC50=18.1083μM | SANGER | |||
| NCI-H1355 | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=18.1318μM | SANGER | |||
| GI-ME-N | Growth inhibition assay | Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=18.453μM | SANGER | |||
| MEL-HO | Growth inhibition assay | Inhibition of human MEL-HO cell growth in a cell viability assay, IC50=18.9753μM | SANGER | |||
| SW982 | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50=19.8406μM | SANGER | |||
| MONO-MAC-6 | Growth inhibition assay | Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=19.9061μM | SANGER | |||
| MFH-ino | Growth inhibition assay | Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=20.2037μM | SANGER | |||
| BEN | Growth inhibition assay | Inhibition of human BEN cell growth in a cell viability assay, IC50=20.3128μM | SANGER | |||
| HT-144 | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay, IC50=20.3697μM | SANGER | |||
| DoTc2-4510 | Growth inhibition assay | Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50=20.7966μM | SANGER | |||
| NCI-H522 | Growth inhibition assay | Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50=20.8971μM | SANGER | |||
| NCI-H1299 | Growth inhibition assay | Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=21.167μM | SANGER | |||
| CAL-12T | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=21.2435μM | SANGER | |||
| CTB-1 | Growth inhibition assay | Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=21.6855μM | SANGER | |||
| COR-L105 | Growth inhibition assay | Inhibition of human COR-L105 cell growth in a cell viability assay, IC50=21.7949μM | SANGER | |||
| NCI-H1650 | Growth inhibition assay | Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50=21.8133μM | SANGER | |||
| SK-MEL-3 | Growth inhibition assay | Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=21.9788μM | SANGER | |||
| 697 | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50=22.0402μM | SANGER | |||
| NEC8 | Growth inhibition assay | Inhibition of human NEC8 cell growth in a cell viability assay, IC50=22.1998μM | SANGER | |||
| ACN | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay, IC50=22.4965μM | SANGER | |||
| MHH-PREB-1 | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=22.5088μM | SANGER | |||
| RPMI-6666 | Growth inhibition assay | Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=22.5905μM | SANGER | |||
| BB30-HNC | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=23.539μM | SANGER | |||
| HOS | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay, IC50=23.8014μM | SANGER | |||
| OVCAR-4 | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=23.984μM | SANGER | |||
| SK-HEP-1 | Growth inhibition assay | Inhibition of human SK-HEP-1 cell growth in a cell viability assay, IC50=24.0791μM | SANGER | |||
| OS-RC-2 | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=24.0858μM | SANGER | |||
| MKN1 | Growth inhibition assay | Inhibition of human MKN1 cell growth in a cell viability assay, IC50=24.1401μM | SANGER | |||
| NCI-H510A | Growth inhibition assay | Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=24.5517μM | SANGER | |||
| DBTRG-05MG | Growth inhibition assay | Inhibition of human DBTRG-05MG cell growth in a cell viability assay, IC50=25.014μM | SANGER | |||
| SW13 | Growth inhibition assay | Inhibition of human SW13 cell growth in a cell viability assay, IC50=25.0254μM | SANGER | |||
| HuO-3N1 | Growth inhibition assay | Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=25.2535μM | SANGER | |||
| U-2-OS | Growth inhibition assay | Inhibition of human U-2-OS cell growth in a cell viability assay, IC50=25.5982μM | SANGER | |||
| PANC-10-05 | Growth inhibition assay | Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50=25.8389μM | SANGER | |||
| NUGC-3 | Growth inhibition assay | Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50=26.0051μM | SANGER | |||
| MZ1-PC | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=26.2821μM | SANGER | |||
| U-118-MG | Growth inhibition assay | Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=26.3272μM | SANGER | |||
| NCI-H1703 | Growth inhibition assay | Inhibition of human NCI-H1703 cell growth in a cell viability assay, IC50=26.4593μM | SANGER | |||
| HT-1080 | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=26.6211μM | SANGER | |||
| EFO-21 | Growth inhibition assay | Inhibition of human EFO-21 cell growth in a cell viability assay, IC50=26.7536μM | SANGER | |||
| TK10 | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay, IC50=27.1653μM | SANGER | |||
| ES1 | Growth inhibition assay | Inhibition of human ES1 cell growth in a cell viability assay, IC50=27.6673μM | SANGER | |||
| DMS-153 | Growth inhibition assay | Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=28.2498μM | SANGER | |||
| KYSE-270 | Growth inhibition assay | Inhibition of human KYSE-270 cell growth in a cell viability assay, IC50=28.3533μM | SANGER | |||
| MLMA | Growth inhibition assay | Inhibition of human MLMA cell growth in a cell viability assay, IC50=28.3719μM | SANGER | |||
| KURAMOCHI | Growth inhibition assay | Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=28.5975μM | SANGER | |||
| NCI-H2347 | Growth inhibition assay | Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50=28.5994μM | SANGER | |||
| MCF7 | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50=28.7093μM | SANGER | |||
| HOP-92 | Growth inhibition assay | Inhibition of human HOP-92 cell growth in a cell viability assay, IC50=28.9327μM | SANGER | |||
| REH | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay, IC50=28.9422μM | SANGER | |||
| RT4 | Growth inhibition assay | Inhibition of human RT4 cell growth in a cell viability assay, IC50=29.2259μM | SANGER | |||
| HT-1197 | Growth inhibition assay | Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=29.2582μM | SANGER | |||
| BL-41 | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay, IC50=29.6923μM | SANGER | |||
| IST-MES1 | Growth inhibition assay | Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=29.8144μM | SANGER | |||
| MOLT-16 | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=30.3744μM | SANGER | |||
| GAK | Growth inhibition assay | Inhibition of human GAK cell growth in a cell viability assay, IC50=31.1007μM | SANGER | |||
| RD | Growth inhibition assay | Inhibition of human RD cell growth in a cell viability assay, IC50=31.2473μM | SANGER | |||
| COR-L23 | Growth inhibition assay | Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=31.3023μM | SANGER | |||
| Capan-2 | Growth inhibition assay | Inhibition of human Capan-2 cell growth in a cell viability assay, IC50=31.6669μM | SANGER | |||
| ALL-PO | Growth inhibition assay | Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=31.9592μM | SANGER | |||
| BCPAP | Growth inhibition assay | Inhibition of human BCPAP cell growth in a cell viability assay, IC50=32.4534μM | SANGER | |||
| OVCAR-3 | Growth inhibition assay | Inhibition of human OVCAR-3 cell growth in a cell viability assay, IC50=32.6497μM | SANGER | |||
| NKM-1 | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=33.1404μM | SANGER | |||
| 647-V | Growth inhibition assay | Inhibition of human 647-V cell growth in a cell viability assay, IC50=33.9321μM | SANGER | |||
| ES5 | Growth inhibition assay | Inhibition of human ES5 cell growth in a cell viability assay, IC50=34.9282μM | SANGER | |||
| A3-KAW | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=35.5285μM | SANGER | |||
| ChaGo-K-1 | Growth inhibition assay | Inhibition of human ChaGo-K-1 cell growth in a cell viability assay, IC50=35.5964μM | SANGER | |||
| NALM-6 | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=35.6045μM | SANGER | |||
| 8-MG-BA | Growth inhibition assay | Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=35.9586μM | SANGER | |||
| BL-70 | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=36.8348μM | SANGER | |||
| MRK-nu-1 | Growth inhibition assay | Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=37.0227μM | SANGER | |||
| COR-L88 | Growth inhibition assay | Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=37.2976μM | SANGER | |||
| MDA-MB-415 | Growth inhibition assay | Inhibition of human MDA-MB-415 cell growth in a cell viability assay, IC50=38.6783μM | SANGER | |||
| Becker | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay, IC50=39.1235μM | SANGER | |||
| NCI-H2452 | Growth inhibition assay | Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=39.1445μM | SANGER | |||
| SW626 | Growth inhibition assay | Inhibition of human SW626 cell growth in a cell viability assay, IC50=39.1841μM | SANGER | |||
| SAS | Growth inhibition assay | Inhibition of human SAS cell growth in a cell viability assay, IC50=39.5476μM | SANGER | |||
| DMS-53 | Growth inhibition assay | Inhibition of human DMS-53 cell growth in a cell viability assay, IC50=39.7553μM | SANGER | |||
| CP66-MEL | Growth inhibition assay | Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=39.7602μM | SANGER | |||
| NCI-H2405 | Growth inhibition assay | Inhibition of human NCI-H2405 cell growth in a cell viability assay, IC50=40.1926μM | SANGER | |||
| MC-CAR | Growth inhibition assay | Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=40.2471μM | SANGER | |||
| CAL-120 | Growth inhibition assay | Inhibition of human CAL-120 cell growth in a cell viability assay, IC50=40.9723μM | SANGER | |||
| GCT | Growth inhibition assay | Inhibition of human GCT cell growth in a cell viability assay, IC50=41.2626μM | SANGER | |||
| A375 | Growth inhibition assay | Inhibition of human A375 cell growth in a cell viability assay, IC50=41.5395μM | SANGER | |||
| MEG-01 | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=41.6116μM | SANGER | |||
| NCI-H2122 | Growth inhibition assay | Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=41.97μM | SANGER | |||
| RPMI-2650 | Growth inhibition assay | Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50=43.4784μM | SANGER | |||
| 8305C | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50=43.7675μM | SANGER | |||
| NCI-H1395 | Growth inhibition assay | Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=44.1055μM | SANGER | |||
| EW-16 | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay, IC50=44.1094μM | SANGER | |||
| T98G | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50=44.4245μM | SANGER | |||
| IST-SL2 | Growth inhibition assay | Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=44.9279μM | SANGER | |||
| NCI-H1651 | Growth inhibition assay | Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=45.9208μM | SANGER | |||
| COR-L279 | Growth inhibition assay | Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=46.2081μM | SANGER | |||
| YT | Growth inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50=46.5067μM | SANGER | |||
| TE-11 | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50=46.7404μM | SANGER | |||
| C-33-A | Growth inhibition assay | Inhibition of human C-33-A cell growth in a cell viability assay, IC50=46.8197μM | SANGER | |||
| OVCAR-5 | Growth inhibition assay | Inhibition of human OVCAR-5 cell growth in a cell viability assay, IC50=47.2307μM | SANGER | |||
| PANC-03-27 | Growth inhibition assay | Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50=47.3513μM | SANGER | |||
| CaR-1 | Growth inhibition assay | Inhibition of human CaR-1 cell growth in a cell viability assay, IC50=48.2474μM | SANGER | |||
| SNU-449 | Growth inhibition assay | Inhibition of human SNU-449 cell growth in a cell viability assay, IC50=49.2285μM | SANGER | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
Informations chimiques, stockage et stabilité
| Poids moléculaire | 437.52 | Formule | C21H23N7O2S |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 444731-52-6 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | GW786034 | Smiles | CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N | ||
Solubilité
|
In vitro |
DMSO
: 87 mg/mL
(198.84 mM)
Water : Insoluble Ethanol : Insoluble |
Calculateur de molarité
Calculateur de dilution
Calculateur de poids moléculaire
|
In vivo |
|||||
Calculateur de formulation in vivo (Solution claire)
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
mg/kg
g
μL
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
Mécanisme daction
| Targets/IC50/Ki |
VEGFR1
(Cell-free assay) 10 nM
VEGFR2
(Cell-free assay) 30 nM
VEGFR3
(Cell-free assay) 47 nM
c-Kit
(Cell-free assay) 74 nM
PDGFR
(Cell-free assay) 84 nM
FGFR
(Cell-free assay) 140 nM
c-Fms
(Cell-free assay) 146 nM
|
|---|---|
| In vitro |
Le Pazopanib inhibe puissamment la phosphorylation du VEGFR2 induite par le VEGF dans les cellules HUVEC avec une IC50 de 8 nM. Ce composé montre une inhibition de la croissance dose-dépendante dans toutes les lignées cellulaires de sarcome synovial, y compris les cellules SYO-1 et HS-SY-II. La prolifération des cellules SYO-1 et HS-SY-II est inhibée même à 1 µg/mL de ce produit chimique et est complètement abolie à 5 µg/mL. Il induit un arrêt en phase G1, et supprime ainsi la croissance des cellules de sarcome synovial. La phosphorylation des Akts, GSK-3β, JNKs, p70 S6 Kinase et mTOR est supprimée dans les cellules SYO-1 traitées avec ce composé par rapport à celles traitées avec le véhicule. Ce produit chimique entre 20 µg/mL et 22,5 µg/mL montre une réduction croissante de la viabilité des cellules RPE. |
| Essai kinase |
Tests enzymatiques de Kinase
|
|
Les essais enzymatiques du VEGFR pour VEGGR1, VEGFR2 et VEGFR3 sont réalisés en format HTRF (Homogeneous Time-Resolved Fluorescence) dans des microplaques à 384 puits en utilisant une protéine de fusion glutathion-S-transférase (GST) purifiée, exprimée par baculovirus, codant pour le c-terminus catalytique des kinases réceptrices VEGFR humaines 1, 2 ou 3. Les réactions sont initiées par l'ajout de 10 μL de solution de kinase VEGFR2 activée [concentration finale, 1 nM d'enzyme dans 0,1 M HEPES, pH 7,5, contenant 0,1 mg/mL d'albumine de sérum bovin (BSA), 300 μM de dithiothréitol (DTT)] à 10 μL de solution de substrat [concentration finale, 360 nM de peptide, (biotin-aminohexyl-EEEEYFELVAKKKK-NH2), 75 μM d'ATP, 10 μM de MgCl2], et 1 μL de ce composé titré dans du DMSO. Les plaques sont incubées à température ambiante pendant 60 minutes, puis la réaction est stoppée par l'ajout de 20 μL d'EDTA 100 mM. Après l'extinction, 20 μL de réactifs HTRF (concentration finale, 15 nM d'allophycocyanine liée à la streptavidine, 1 nM d'anticorps anti-phosphotyrosine marqué à l'europium dilué dans 0,1 mg/mL de BSA, 0,1 M HEPES, pH 7,5) sont ajoutés et les plaques sont incubées pendant au moins 10 minutes. La fluorescence à 665 nM est mesurée avec un lecteur de plaques Wallac Victor en utilisant un délai de 50 μs.
|
|
| In vivo |
Les souris traitées avec 30 mg/kg ou 100 mg/kg de Pazopanib révèlent une diminution significative de la charge tumorale par rapport aux souris traitées avec le véhicule ou 10 mg/kg de ce composé. Le traitement avec cet agent est bien toléré et il n'y a pas de différence significative de poids corporel entre les souris de chaque groupe. |
Références |
|
Applications
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | p-Akt / Akt p53 / PUMA |
|
27924057 |
| Growth inhibition assay | Cell viability |
|
27924057 |
Informations sur lessai clinique
(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | 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 |
Support technique
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Les produits sont destinés à la recherche uniquement. Ne pas utiliser chez lhomme. Nous ne vendons pas aux patients.
©Copyright 2013 Selleck Chemicals. Tous droits réservés.