Chemical Structure : TAS-115
CAS No.: 1190836-34-0
Catalog No.: 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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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.
M.Wt | 518.563 | |
Formula | C27H23FN4O4S | |
Appearance | Solid | |
Storage |
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Solubility |
100 mM in DMSO (51.8 mg/mL) |
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Chemical Name/SMILES |
4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy] -7-methoxy-N-methyl-6-quinolinecarboxamide |
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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