TAS0728 产品说明书 Chemicals
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产品编号 DC22243
名称 TAS0728

化学性质

CAS 2088323-16-2
分子式 C26H32N8O3
分子量 504.595
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description TAS0728 是一种有效、选择性、可口服、不可逆、共价结合的 HER2 抑制剂,与 HER2 的 C805 位点共价结合,抑制其活性,IC50 值为 13 nM。TAS0728 对 BMX,HER4,BLK,EGFR,JAK3,SLK,LOK 和 人 HER2 的 IC50 值分别为 4.9,8.5,31,65,33,25,86 和 36 nM。TAS0728 同时可抑制 HER2,HER3 及其下游效应蛋白的磷酸化。具有抗肿瘤活性。
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


TAS0728 (TAS-0728, TAS 0728) is a potent, selective, covalent, orally available inhibitor of HER2 kinase with IC50 of 36 nM in in vitro kinase assays; covalently binds to the recombinant human HER2 cytoplasmic domain, modified cysteine residue C805; inhibits EGFR recombinant with IC50 of 65 nM, shows excellent selectivity in a panel of 374 kinases; strongly inhibits the phosphorylation of HER2 in SK-BR-3 cells at 30-1000 nM, with weakly inhibition on phosphorylation of EGFR; potently inhibited the in vitro proliferation of five HER2-amplified cell lines with GI50 of <10 nM, exhibited robust and sustained inhibition of the phosphorylation of HER2, HER3; induced tumor regression in mouse xenograft models bearing HER2 signal-dependent tumors and exhibited a survival benefit without any evident toxicity.Solid TumorsPhase 2 Clinical
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