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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-TAS0728
TAS0728

Chemical Structure : TAS0728

CAS No.: 2088323-16-2

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TAS0728 (TAS-0728;TAS 0728)

货号: PC-36109Not For Human Use, Lab Use Only.

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.

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25 mg ￥4680 In stock
50 mg ￥7880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
TAS0728 covalently binds to the recombinant human HER2 cytoplasmic domain, modified cysteine residue C805.
TAS0728 inhibits EGFR recombinant with IC50 of 65 nM, shows excellent selectivity in a panel of 374 kinases.
TAS0728 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.
TAS0728 induced tumor regression in mouse xenograft models bearing HER2 signal-dependent tumors and exhibited a survival benefit without any evident toxicity.

物理化学性质&存储条件

分子量 504.595
分子式 C26H32N8O3
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

10 mM in DMSO
Chemical Name/SMILES

(R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide

参考文献

1. Irie H, et al. Mol Cancer Ther. 2019 Feb 20. pii: molcanther.1085.2018.

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