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JAK1-IN-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JAK1-IN-3图片
CAS NO:2091134-68-6
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
JAK1-IN-3 (AZD4205) 是一种选择性 JAK1 抑制剂,IC50 为 73 nM,弱抑制 JAK2 (IC50>14.7 μM),对 JAK3 几乎没有抑制作用 (IC50>30 μM)。
Cas No.2091134-68-6
别名Golidocitinib; AZD4205
Canonical SMILESC[C@@H](N1CCN(C)CC1)C(NC2=C3C(C(C4=NC(NC5=CN(C)N=C5OC)=NC=C4)=CN3)=CC=C2)=O
分子式C25H31N9O2
分子量489.57
溶解度DMSO: 250 mg/mL (510.65 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JAK1-IN-3 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively).

JAK1-IN-3 (Example 32) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively). JAK1-IN-3 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC50 of 161 nM[1].

JAK1-IN-3 (12.5 mg/kg BID (twice daily), 25 m/kg BID or 50 mg/kg BID, p.o.) alone has increasing antitumor effects, and ehances the antitumor activity of osimertinib, compared to treatment with osimertinib alone in mice bearing NCI-H1975 cells[1].

[1]. Annika Birgitta Margareta ?STRAND, et al. Compounds and methods for inhibiting jak.