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JAK3-IN-1
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。
JAK3-IN-1图片
CAS NO:1805787-93-2
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
JAK3-IN-1是一种有效的JAK3抑制剂,IC50值为4.8nM,也能抑制JAK1(IC50=896nM)和JAK2(IC50=1050nM)。
Cas No.1805787-93-2
Canonical SMILESO=C(C=C)NC1=CC(CNC2=NC(NC3=C(OC)C=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=CC=C1
分子式C26H30ClN7O2
分子量508.02
溶解度DMSO : ≥ 47 mg/mL (92.52 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

JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).IC50 value: 4.8 nM [1]Target: JAK3in vitro: JAK3-IN-1 provides a set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. In a similar way, JAK3-IN-1 exhibits consistent potency and selectivity for JAK3 in leukemia cancer cell lines: TALL-1 and OCL-AML5. [1]in vivo: JAK3-IN-1 demonstrates reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng.h/mL following a 10 mg/kg oral dose and good oralbioavailability of 66%. [1]

[1]. Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.