| Name | Pamufetinib |
| Description | Pamufetinib (TAS-115) is a potent kinase inhibitor targeting VEGFR and the hepatocyte growth factor receptor (c-Met/HGFR), with IC50s of 30 nM for rVEGFR2 and 32 nM for rMET, respectively. |
| In vitro | pamufetinib is ATP antagonism(Ki of 12 and 39 nM for rVEGFR2 and rMET, respectively). Like other known VEGFR or MET inhibitors, AS-115 strongly inhibits the kinase activity of VEGFR2 and MET and their signal-dependent cell growth. TAS-115 induces less damage in various normal cells than do other VEGFR inhibitors[1]. TAS-115 does not affect the growth of PC-9 or HCC827 cells at concentrations less than 10 μM; however, the combined use of TAS-115 with erlotinib reverses HGF-induced resistance in the cell lines in a concentration-dependent manner. VEGF production by cancer cells and endothelial proliferation inhibited by TAS-115[2]. |
| In vivo | During the treatment period,pamufetinib (50 mg/kg/d) completely prevents tumor growth. In MET-amplified human cancer transplanted models,pamufetinib (200 mg/kg/d) induces a 48% regression from the initial tumor volume . ED50 of Tpamufetinib in this model is 8 mg/kg/d. Pamufetinib significantly prolongs survival of these mice when administered at doses of 50 or 200 mg/kg/d[1]. Pamufetinib inhibits angiogenesis in PC-9/HGF tumors in vivo. Moreover, the doublet erlotinib and pamufetinib successfully inhibit PC-9/HGF tumor growth and delay tumor regrowth associated with sustained tumor vasculature inhibition even after cessation of the treatment[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 13 mg/ml (25.07 mM)
|
| Keywords | c-Met/HGFR | Inhibitor | TAS 115 | Pamufetinib | inhibit | TAS115 | VEGFR | Vascular endothelial growth factor receptor |
| Inhibitors Related | Ribociclib | Nintedanib | Regorafenib monohydrate | Sorafenib | L-Ascorbic acid 2-phosphate trisodium | Regorafenib | Sorafenib tosylate | Lenvatinib mesylate | Pazopanib | Axitinib |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Anti-Prostate Cancer Compound Library | Bioactive Compounds Library Max |
United States
