产品详情
简单介绍：
CP-690550,JAKInhibitor
详情介绍：
Product Information
| Chemical Name: | 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile |
| Molecular Weight: | 312.38 |
| Formula: | C16H20N6O |
| Purity: | ≥ 98% |
| CAS#: | 477600-75-2 |
| Solubility: | DMSO up to 100 mM |
| Storage: | Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year |
Biological Activity:
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).
How to Use:
- In vitro: CP-690550 was used at 0.05-1 µM concentration in a panel of in vitro assays.
- In vivo: CP-690550 was orally dosed to rats at 10-50 mg/kg once or twice per day.
Reference:
- 1. 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
- 2. Meyer DM, et al. Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis. (2010) J Inflamm (Lond).11;7:41.
- 3. Ghoreschi K, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). (2011) J Immunol. 186(7):4234-43.
- 4. 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.
- Product Specification:
- Product MSDS:
Products are for research use only. Not for human use.
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