Tasocitinib(CP-690550) JAKs选择性抑制剂

保质期 ：2 years

英文名 ：Tofacitinib

库存 ：10

供应商 ：上海伟进生物科技有限公司

CAS号 ：477600-75-2

保存条件 ：-20℃

规格 ：10mg

Biological Activity

Tofacitinib (CP-690550) is a potent, selective, and ATP-competitive JAK inhibitor, suppressing all four JAK isoforms with nM potency in vitro enzyme assays (IC₅₀ values are 3.2 nM, 4.1 nM, 1.6 nM, and 34 nM for JAK1, JAK2, JAK3, and TYK2, respectively), but significantly inhibiting signaling through JAK1 and JAK3 with 5-100 fold selectivity over JAK2 in cellular assays. This agent is being developed as an immunosuppressive and anti-inflammatory drug for the treatment and prevention of acute allograft rejection, RA, psoriasis and other immune mediated diseases ^[1]. CP-690550 shows great efficacy in various rodent and nonhuman primate models of allograft organ transplantation ^[2-4], as well as rodent models of RA ^{[1, 5]}.

Chemical Properties

Cas No.: 477600-75-2	M. Wt.: 312.37
Formula: C16H20N6O	Purity: >99%
Synonym: CP-690550, CP-690,550, Tasocitinib
Chemical Name: 3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
Appearance: Off-white to pale yellow solid
Solubility: Soluble in DMSO up to 100 mM
Storage: Store solid at -20 ºC for the stability of two years

Application Concentration (Just for reference)

The appropriate working concentration of Tofacitinib depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.