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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-AZD 4205
AZD 4205

Chemical Structure : AZD 4205

CAS No.: 2091134-68-6

AZD 4205 (AZD4205, Golidocitinib)

货号: PC-61986Not For Human Use, Lab Use Only.

Golidocitinib (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively.

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

生物&药学活性

Golidocitinib (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively.
Golidocitinib (AZD4205) shows 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.
Golidocitinib (AZD4205) reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

物理化学性质&存储条件

分子量 521.601
分子式 C25H31N9O2
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

(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

参考文献

1. Jason G. Kettle, et al. AACR Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205.

2.  Patent: WO 2017050938 A1 20170330, Example 32.

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