AZD 4205 产品说明书 Chemicals
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产品编号 DC20726
名称 AZD 4205

化学性质

CAS 2091134-68-6
分子式 C25H31N9O2
分子量 521.601
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
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


AZD4205 (AZD-4205) is a potent, selective and ATP-competitive inhibitor of JAK1 with a Ki of 2.8 nM, highly selective against JAK2 (IC50 =13233 nM, >4000 fold selectivity) and JAK3 (IC50 >30000 nM, >10000 fold selectivity). Demonstrates potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome. Exhibits excellent pharmacokinetics, and in vitro and in vivo antitumor efficacy (refs 1, 2), and is currently in clinical evaluation.
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