CP-690550 is a potent and selective JAK inhibitor currently in clinical trials for rheumatoid arthritis (RA) and other autoimmune disease indications. It inhibits recombinant human JAK1 (IC50 ~ 3.2 nM), JAK2 (IC50 ~4.1 nM), and JAK3 (IC50 ~1.6 nM). In cellular assays CP-690550 showed potent effects in the IL-2 blast proliferation assay (IC50 ~11 nM, mediated via JAK1 and JAK3) and HU03 cellular specificity assay (IC50 ~324 nM, mediated via JAK2), but has relatively minimal effects on general cell growth (>10 µM activity in the HFF assay).
CAS Number: 477600-75-2
Molecular Weight: 312.37
Chemical Name: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
CP-690550 was used at 0.05-1 µM concentration in a panel of in vitro assays.
CP-690550 was orally dosed to rats at 10-50 mg/kg once or twice per day.
- Flanagan ME, et al. Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. (2010) J Med Chem. 53(24):8468-84
- Ghoreschi K, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). (2011) J Immunol. 186(7):4234-43.
- Ju W, et al. CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP. (2011) Blood. 117(6):1938-46.
Products are for research use only. Not for human use.
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