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CAS No.: 944842-54-0

Decernotinib Catalog No. CSN13843

Synonyms: VX-509;VRT-831509;Adelatinib

Decernotinib is a selective JAK3 inhibitor with Ki value of 2.5nM, with >4-fold selectivity over JAK1, JAK2, and TYK2 with Ki values of 11nM, 13nM and 13nM, respectively.

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实验方案

技术信息

生物活性

描述Janus kinases (JAKs) includes cytokines, growth factors, and other chemical messengers rely on a class of intracellular nonreceptor tyrosine kinases can rapidly transduce intracellular signals. Targeting the Janus tyrosine kinases (JAKs), which play essential roles in cell signaling responses and can contribute to aberrant immune function associated with disease, has emerged as a novel and attractive approach for the development of new autoimmune disease therapies. JAK3 is of particular interest due to its importance in immune function and its expression, which is largely confined to lymphocytes, thus limiting the potential impact of JAK3 inhibition on nonimmune physiology. JAK-STAT dysregulation results in autoimmune disorders such as rheumatoid arthritis, ulcerative colitis, and Crohn disease^[3]. Decernotinib （VX-509） potently inhibits JAK3 in enzyme assays with Ki of 2.5 nM and cellular assays dependent on JAK3 activity with IC₅₀ ranging from 50-170 nM. JAK3 inhibition by VX-509 was determined with an (interleukin) IL-2-induced STAT-5 phosphorylation assay in an IL-2-dependent T-cell line (HT-2). In the IL-2-stimulated HT-2-phosphorylated STAT-5 fluorescence-activated cell sorting assay, VX-509 had an IC₅₀ of 99 ± 40 nM. VX-509 showed statistically significant, dose-dependent inhibition of the increases in ankle diameter and paw weight that occur in response to collagen injections in rats treated with VX-509 b.i.d. at doses of 10, 25, or 50 mg/kg or etanercept at 10 mg/kg. Inhibition of ankle diameter increase was significant with VX-509 at 10 mg/kg b.i.d. (55% inhibition), 25 mg/kg b.i.d. (70% inhibition), 50 mg/kg b.i.d. (76% inhibition), or 10 mg/kg etancercept (55% inhibition) relative to collagen plus vehicle-treated rats^[4].
作用机制Decernotinib can bind to ATP binding pockets of JAK2 with hinge hydrogen bonds to Leu 932.
参考文献

[1] Mahajan S, Hogan JK, et al. VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther. 2015 May;353(2):405-14.
[2] Farmer LJ, Ledeboer MW, et al. Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases. J Med Chem. 2015 Sep 24;58(18):7195-216.
[3] Roskoski R Jr. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Sep;111:784-803. doi: 10.1016/j.phrs.2016.07.038. Epub 2016 Jul 26. PMID: 27473820.
[4] Mahajan S, Hogan JK, Shlyakhter D, Oh L, Salituro FG, Farmer L, Hoock TC. VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther. 2015 May;353(2):405-14. doi: 10.1124/jpet.114.221176. Epub 2015 Mar 11. PMID: 25762693.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5486 mL
- 12.7428 mL
- 25.4856 mL
- 5 mM
- 0.5097 mL
- 2.5486 mL
- 5.0971 mL
- 10 mM
- 0.2549 mL
- 1.2743 mL
- 2.5486 mL

技术信息

CAS号

944842-54-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H19F3N6O

运输

蓝冰

分子量

392.38

别名

VX-509;VRT-831509;Adelatinib

溶解度

DMSO	175.0 mg/mL (446.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	3.5 mg/mL	clear
PO	0.5% CMC-Na	42 mg/mL	suspension

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