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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-JAK1 inhibitor AZ-3
JAK1 inhibitor AZ-3

Chemical Structure : JAK1 inhibitor AZ-3

CAS No.: 2228908-91-4

JAK1 inhibitor AZ-3

货号: PC-26419Not For Human Use, Lab Use Only.

JAK1 inhibitor AZ-3 is a potent, selective and orally efficacious JAK1 inhibitor with IC50 of 3.4 nM, >1000-fold selective over JAK2 , JAK3 and TYK2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JAK1 inhibitor AZ-3 is a potent, selective and orally efficacious JAK1 inhibitor with IC50 of 3.4 nM, >1000-fold selective over JAK2 , JAK3 and TYK2.
AZ-3 exhibits potent inhibition of pSTAT3 in NCI-H1975 cells with IC50 of 30 nM.
AZ-3 (1, 3, 10, 30, 50, and 100 mg/kg, oral gavage) induced a dose-dependent decrease in pSTAT3 in NCI-H1975 mouse xenograft model.

物理化学性质&存储条件

分子量 385.49
分子式 C20H28FN7
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

N4-((R)-sec-butyl)-N2-(2-fluoro-5-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)pyridin-3-yl)-5-methylpyrimidine-2,4-diamine

参考文献

1. Grimster NP, et al. J Med Chem. 2018 Jun 28;61(12):5235-5244.

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