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首页-小分子抑制剂&激动剂-Tyrosine Kinase-VEGFR-TAS-115
TAS-115

Chemical Structure : TAS-115

CAS No.: 1190836-34-0

TAS-115 (Pamufetinib, TAS115)

货号: PC-63554Not For Human Use, Lab Use Only.

TAS-115 (Pamufetinib) is a potent, dual VEGFR2/c-Met inhibitor with IC50 of 30 and 32 nM against rVEGFR2 and rMET, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TAS-115 (Pamufetinib) is a potent, dual VEGFR2/c-Met inhibitor with IC50 of 30 and 32 nM against rVEGFR2 and rMET, respectively.
TAS-115 also inhibits PDGFRα/β, Axl, c-Kit, Src, FLT-1 in a 192-kinase panel assay.
TAS-115 markedly inhibits the tyrosine phosphorylation of VEGFR2 at 10 nM in VEGF-stimulated HUVECs, also inhibits the tyrosine phosphorylation of MET in MKN45 cells.
TAS-115 inhibits cellular proliferation of HUVECs under VEGF-dependent growth condition with IC50 of 19 nM, with weak inhibition of growth (GI50>10 uM) in VEGFR signal- or MET signal-independent cells.
TAS-115 effectively suppresses the progression of MET-inactivated tumor by blocking angiogenesis in vivo.

物理化学性质&存储条件

分子量 518.563
分子式 C27H23FN4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

100 mM in DMSO (51.8 mg/mL)

Chemical Name/SMILES

4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy] -7-methoxy-N-methyl-6-quinolinecarboxamide

参考文献

1. Fujita H, et al. Mol Cancer Ther. 2013 Dec;12(12):2685-96.

2. Kunii E, et al. Anticancer Res. 2015 Oct;35(10):5241-7.

3. Fujita H, et al. PLoS One. 2016 Oct 13;11(10):e0164830.

4. Yamada S, et al. BMC Cancer. 2017 May 16;17(1):334.

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