CP-690550 --- JAK Inhibitor


Catalog No. size PriceQuantity
M60033-2D 10 mM in DMSO (0.641 mL) $79
M60033-2S 2 mg solid $79
M60033-25S 25 mg solid $550

Description

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).

Product information

CAS Number: 477600-75-2

Molecular Weight: 312.37

Formula: C16H20N6O

Synonym:

Tofacitinib

tasocitinib

Chemical Name: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile

Smiles: CN([C@H]1CN(CC[C@H]1C)C(=O)CC#N)C1N=CN=C2NC=CC2=1

InChiKey: UJLAWZDWDVHWOW-YPMHNXCESA-N

InChi: InChI=1S/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1

Technical Data

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

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.

References:

  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. Ghoreschi K, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). (2011) J Immunol. 186(7):4234-43.
  3. 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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