(3R,4S)-Tofacitinib

CAS Number: 1092578-46-5


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Cat No.: 1092578-46-5
Biological Description:
Tofacitinib(CP-690550) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
IC50 value: 1 nM [1]
Target: JAK3
in vitro: CP-690550 is a specific, orally inhibitor of JAK3, it is 20- to 100-fold less potent for JAK2 and JAK1 with IC50 of 20 nM and 112 nM, respectively. CP-690550 doesn't have potent activity against 30 other kinases (all median IC50 > 3000 nM). CP-690,550 inhibits IL-2–induced proliferation with 30-fold greater potency than its effects on GM-CSF–induced proliferation [1]. CP-690550 effectively inhibits a murine mixed lymphocyte reaction (MLR) (IC50 = 91 nM) [2]. CP-690550 potently inhibits IL-4 induced upregulation of CD23 (IC50=57 nM) and class II major histocompatibility complex (MHCII) expression (IC50=71 nM) on murine B cells [3].
in vivo: In a murine model of heterotopic heart transplantation (DBA2 donor heart into C57/BL6 host), CP-690550 results in a dose-dependent increase in survival of transplanted hearts.The EC50 (drug concentrati...

Purity: >98%

Molecular formula: C16H20N6O

Molecular Weight: 312.37

Storage Instructions: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

References: for more information, please visit http://www.ncbi.nlm.nih.gov