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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-AZ14133346
AZ14133346

Chemical Structure : AZ14133346

CAS No.:

AZ14133346 (AZ 14133346, AZ-14133346)

货号: PC-22389Not For Human Use, Lab Use Only.

AZ14133346 is a potent and selective inhibitor of EGFR Ex20Ins with enzyme IC50 of <3 nM and cell IC50 of 85 nM, 14-fold selective over wild-type EGFR (cell IC50=1200 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AZ14133346 is a potent and selective inhibitor of EGFR Ex20Ins with enzyme IC50 of <3 nM and cell IC50 of 85 nM, 14-fold selective over wild-type EGFR (cell IC50=1200 nM).
AZ14133346 is both a potent and efficacious inhibitor of EGFR Ex20Ins and has an improved in vivo margin to WT when compared to CLN-081.
AZ14133346 can achieve robust Ex20Ins-mediated pathway inhibition in H2073 Ex20Ins SVD (D770_N771InsSVD) xenograft models.

物理化学性质&存储条件

分子量 477.57
分子式 C29H27N5O2
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

(S,E)-1-(3-(3-(3-(2-(5-Cyclopropyloxazol-2-yl)vinyl)phenyl)-4-(pyridin-4-yl)-1H-pyrazol-1-yl)pyrrolidin-1-yl)prop-2-en-1-one

参考文献

1. Clare Thomson, et al. Journal of Medicinal Chemistry, May 21, 2024.

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