JAK3-IN-1 |
| カタログ番号GC33046 |
JAK3-IN-1 は、4.8 nM の IC50 を持つ強力で選択的な経口活性 JAK3 阻害剤です。 JAK3-IN-1 は、JAK1 (896 nM の IC50) および JAK2 (1050 nM の IC50) よりも JAK3 に対して 180 倍以上の選択性を示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1805787-93-2
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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