solo per uso di ricerca
Pazopanib VEGFR inibitore
N. Cat.S3012
Struttura chimica
Peso molecolare: 437.52
Vai a
Controllo Qualità
Lotto:
Purezza:
99.98%
99.98
| Target correlati | EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit |
|---|---|
| Altro VEGFR Inibitori | SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 ZM 323881 HCl |
Coltura cellulare, trattamento e concentrazione di lavoro
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | 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 | |||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
Informazioni chimiche, conservazione e stabilità
| Peso molecolare | 437.52 | Formula | C21H23N7O2S |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 444731-52-6 | Scarica SDF | Conservazione delle soluzioni stock |
|
|
| Sinonimi | 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 | ||
Solubilità
|
In vitro |
DMSO
: 87 mg/mL
(198.84 mM)
Water : Insoluble Ethanol : Insoluble |
Calcolatore di Molarità
Calcolatore di Diluizione
Calcolatore del Peso Molecolare
|
In vivo |
|||||
Calcolatore di formulazione in vivo (Soluzione chiara)
Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
mg/kg
g
μL
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
Meccanismo dazione
| 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 |
Pazopanib inibisce potentemente la fosforilazione di VEGFR2 indotta da VEGF nelle cellule HUVEC con una IC50 di 8 nM. Questo composto mostra un'inibizione della crescita dose-dipendente in tutte le linee cellulari di sarcoma sinoviale, incluse le cellule SYO-1 e HS-SY-II. La proliferazione delle cellule SYO-1 e HS-SY-II è inibita anche a 1 µg/mL di questa sostanza chimica ed è completamente abolita a 5 µg/mL. Induce l'arresto in fase G1, e quindi sopprime la crescita delle cellule di sarcoma sinoviale. La fosforilazione di Akts, GSK-3β, JNKs, p70 S6 Kinase e mTOR è soppressa nelle cellule SYO-1 trattate con questo composto rispetto a quelle trattate con il veicolo. Questa sostanza chimica tra 20 µg/mL e 22,5 µg/mL mostra una crescente riduzione della vitalità delle cellule RPE. |
| Saggio chinasico |
Saggi enzimatici di Kinase
|
|
I saggi enzimatici VEGFR per VEGGR1, VEGFR2 e VEGFR3 sono eseguiti in formato di fluorescenza a risoluzione temporale omogenea (HTRF) in micropiastre a 384 pozzetti utilizzando una proteina di fusione glutatione-S-transferasi (GST) purificata ed espressa in baculovirus che codifica il C-terminale catalitico delle chinasi recettoriali VEGFR umane 1, 2 o 3. Le reazioni sono iniziate con l'aggiunta di 10 μL di soluzione di chinasi VEGFR2 attivata [concentrazione finale, 1 nM di enzima in 0,1 M HEPES, pH 7,5, contenente 0,1 mg/mL di albumina di siero bovino (BSA), 300 μM di ditiotreitolo (DTT)] a 10 μL di soluzione di substrato [concentrazione finale, 360 nM di peptide, (biotin-aminoesil-EEEEYFELVAKKKK-NH2), 75 μM di ATP, 10 μM di MgCl2], e 1 μL di questo composto titolato in DMSO. Le piastre sono incubate a temperatura ambiente per 60 minuti, e quindi la reazione è interrotta con l'aggiunta di 20 μL di 100 mM di acido etilendiamminotetraacetico (EDTA). Dopo l'interruzione, vengono aggiunti 20 μL di reagenti HTRF (concentrazione finale, 15 nM di alloficocianina legata a streptavidina, 1 nM di anticorpo anti-fosfotirosina marcato con europio diluito in 0,1 mg/mL di BSA, 0,1 M HEPES, pH 7,5) e le piastre vengono incubate per un minimo di 10 minuti. La fluorescenza a 665 nM è misurata con un lettore di piastre Wallac Victor utilizzando un ritardo di tempo di 50 μs.
|
|
| In vivo |
I topi trattati con 30 mg/kg o 100 mg/kg di Pazopanib rivelano una significativa diminuzione del carico tumorale rispetto ai topi trattati con veicolo o 10 mg/kg di questo composto. Il trattamento con questo agente è ben tollerato e non vi è alcuna differenza significativa nel peso corporeo tra i topi di ciascun gruppo. |
Riferimenti |
|
Applicazioni
| Metodi | Biomarcatori | Immagini | PMID |
|---|---|---|---|
| Western blot | p-Akt / Akt p53 / PUMA |
|
27924057 |
| Growth inhibition assay | Cell viability |
|
27924057 |
Informazioni sullo studio clinico
(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| 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 |
Supporto tecnico
Istruzioni per la manipolazione
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