Pamufetinib (TAS-115) mesylate是一种有效的 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 32 nM。

Pamufetinib (TAS-115) mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC 50 s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

Solid

IC50: 30 nM (rVEGFR2), 32 nM (rMET)

Pamufetinib mesylate 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. Pamufetinib mesylate has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors. Crizotinib and Pamufetinib mesylate inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

Pamufetinib mesylate 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 Pamufetinib mesylate. Pamufetinib mesylate induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 75 mg/mL (122.02 mM; Need ultrasonic)配制储备液