TAS-115mesylate是一种有效的血管内皮生长因子(VEGFR)和肝细胞生长因子受体(c-Met/HGFR)的靶向激酶抑制剂，能够抑制rVEGFR2和rMET的活性，IC50值分别为30和32nM。
CAS：1688673-09-7
分子式：C28H27FN4O7S2
分子量：614.66
纯度：98%
存储：Store at -20°C

Background:

TAS-115 mesylate is a potent vascular endothelial growth factor (VEGFR) and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI50=0.032-0.362 μM) as a MET-targeted inhibitor. TAS-115 has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors[1]. Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells[2].

TAS-115 completely suppresses the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer-bearing mice[1].

[1]. Fujita H, et al. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile. Mol Cancer Ther. 2013 Dec;12(12):2685-96. [2]. Nakade J, et al. Triple inhibition of EGFR, Met, and VEGF suppresses regrowth of HGF-triggered, erlotinib-resistant lung cancer harboring an EGFR mutation. J Thorac Oncol. 2014 Jun;9(6):775-83.