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Pamufetinib

CAS No. : 1190836-34-0

MCE 站：Pamufetinib

产品活性：Pamufetinib (TAS-115) 是一种有效的 VEGFR 和 c-Met/HGFR 抑制剂，能够抑制 rVEGFR2 和 rMET 的活性，IC₅₀ 值分别为 30 和 32 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR  |  c-Met/HGFR

In Vitro: Pamufetinib is ATP antagonism with inhibition constant (K_i) values against rVEGFR2 and rMET of 12 and 39 nM, respectively. Pamufetinib inhibits the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. Pamufetinib induces less damage in various normal cells than do other VEGFR inhibitors. Pamufetinib does not affect the growth of PC-9 or HCC827 cells at concentrations less than 10 μM; however, the combined use of Pamufetinib with erlotinib reverses HGF-induced resistance in the cell lines in a concentration-dependent manner. Pamufetinib inhibits VEGF production by cancer cells and endothelial proliferation.

In Vivo: Pamufetinib (50 mg/kg/d) completely prevents tumor growth during the treatment period. Pamufetinib (200 mg/kg/d) induces a 48% regression from the initial tumor volume in MET-amplified human cancer transplanted models. The estimated 50% effective dose (ED₅₀) of Pamufetinib 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. 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.

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