TAS-115 mesylate (TAS-115 methanesulfonate)

产品编号: DC12256 Featured
TAS-115 mesylate (TAS-115 methanesulfonate)
结构式
1688673-09-7
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中国地区超过5000个高品质化合物库存
应用领域
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。
Cas No.: 1688673-09-7
名称:
别名: TAS115,TAS 115
SMILES: CS(=O)(O)=O.O=C(C1=C(OC)C=C2N=CC=C(OC3=CC=C(NC(NC(CC4=CC=CC=C4)=O)=S)C=C3F)C2=C1)NC
分子式: C28H27FN4O7S2
分子量: 614.66
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: In Vitro TAS-115 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. TAS-115 has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors. Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells. In Vivo TAS-115 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 TAS-115. TAS-115 induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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