1805787-93-2

1805787-93-2 structure

Name: JAK3-IN-1
Chemical Name: JAK3-IN-1
CAS Number: 1805787-93-2
Molecular Formula: C₂₆H₃₀ClN₇O₂
Molecular Weight: 508.015
Catalog: Research Areas Cancer
Create Date: 2018-03-30 06:07:54
Modify Date: 2024-01-14 18:01:05
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]

Name	JAK3-IN-1
Synonyms	N-(3-{[(5-Chloro-2-{[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)amino]methyl}phenyl)acrylamide N-(3-{[(5-Chloro-2-{[2-Methoxy-4-(4-Methylpiperazin-1-Yl)phenyl]amino}pyrimidin-4-Yl)amino]methyl}phenyl)prop-2-Enamide 2-Propenamide, N-[3-[[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]methyl]phenyl]-

Description	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]
Related Catalog	Research Areas >> Cancer
Target	JAK3:4.8 nM (IC50) JAK1:896 nM (IC50) JAK2:1050 nM (IC50) TTK:49 nM (IC50) BTK:794 nM (IC50) ITK:1070 nM (IC50)
References	[1]. Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.