AZD 4205

产品编号: DC20726 Featured
AZD 4205
结构式
2091134-68-6
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中国地区超过5000个高品质化合物库存
应用领域
JAK1-IN-3 是一种选择性的 JAK1 抑制剂,IC50 值为 73 nM,对 JAK2 的抑制作用较弱,对 JAK3 的抑制作用很小,IC50 值分别为 >14.7,>30 μM。
Cas No.: 2091134-68-6
名称: (R)-N-(3-(2-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide
别名: AZD4205,AZD-4205
SMILES: O=C([C@@H](C)N1CCN(C)[C@H](C)C1)NC2=CC=CC3=C2NC=C3C4=C(F)C=NC(NC5=CN(C)N=C5OC)=N4
分子式: C25H31N9O2
分子量: 521.601
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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