產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 20mg
CAS	1190836-34-0
別名	N/A
化學(xué)名	N/A
分子式	C27H23FN4O4S
分子量	518.56
溶解度	Soluble in DMSO
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

TAS-115 is a potent 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 is ATP antagonism with inhibition constant (Ki) values against rVEGFR2 and rMET of 12 and 39 nM, respectively. AS-115 inhibits the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. 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. TAS-115 inhibits VEGF production by cancer cells and endothelial proliferation[2].

TAS-115 (50 mg/kg/d) completely prevents tumor growth during the treatment period. TAS-115 (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 TAS-115 in this model is 8 mg/kg/d. TAS-115 significantly prolongs survival of these mice when administered at doses of 50 or 200 mg/kg/d[1]. TAS-115 inhibits angiogenesis in PC-9/HGF tumors in vivo. Moreover, the doublet erlotinib and TAS-115 successfully inhibit PC-9/HGF tumor growth and delay tumor regrowth associated with sustained tumor vasculature inhibition even after cessation of the treatment[2].

[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.

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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