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

Chemical Structure : Theliatinib

CAS No.: 1353644-70-8

Theliatinib (HMPL309, HMPL-309)

货号: PC-62121Not For Human Use, Lab Use Only.

Theliatinib (HMPL309) is a highly selective, potent, ATP-competitive inhibitor of EGFR with IC50 of 3 nM/22 nM for EGFR/EGFRT790M/L858R mutant, respectively.

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

生物&药学活性

Theliatinib (HMPL309) is a highly selective, potent, ATP-competitive inhibitor of EGFR with IC50 of 3 nM/22 nM for EGFR/EGFRT790M/L858R mutant, respectively.
Theliatinib (HMPL309) demonstrates 50-fold greater selectivity for EGFR compared to 72 other kinases.
Theliatinib (HMPL309) inhibits EGFR phosphorylation (IC50=7 nM) and cell survival in tumor cells
Theliatinib (HMPL309) shows in vivo activity in multiple xerographs such as A-431, Bcap-37 and Fadu; generally well tolerated in animals and orally bioactive.

物理化学性质&存储条件

分子量 442.523
分子式 C25H26N6O2
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

(3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide

参考文献

1. Ren Y, et al. Oncotarget. 2017 Apr 19;8(31):50832-50844.

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