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Tofacitinib (CP-690550) Citrate

Potent JAK inhibitor

Tofacitinib (CP-690550) Citrate

Catalog No. A4135
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
10mg $90.00 In stock
50mg $290.00 In stock

All inclusive: Shipping and all other fees included

Tel: +1-832-696-8203

Email: sales@apexbt.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Tofacitinib (CP-690550) Citrate

Related Biological Data

Tofacitinib (CP-690550) Citrate

Related Biological Data

Tofacitinib (CP-690550) Citrate

Biological Activity

Targets JAK3          
IC50 1 nM          

Tofacitinib (CP-690550) Citrate Dilution Calculator

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Chemical Properties

Cas No. 540737-29-9 SDF Download SDF
Synonyms Tasocitinib citrate,CP 690550 citrate
Chemical Name 2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
Canonical SMILES CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Formula C16H20N6O.C6H8O7 M.Wt 504.49
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

Tofacitinib citrate, also known as CP-690550 citrate, is a potent inhibitor of janus kinase 3 (JAK3), a hematopoetic cell-restricted tyrosine kinase involved in signal transduction regulating lymphocyte survival, proliferation, differentiation, and apoptosis.  The inhibition is JAK3 specific with a selectivity 1000-fold more than other non-JAK family kinases. Besides inhibiting JAKS (IC50 = 1 nM), tofacitinib citrate also inhibits janus kinase 2 (JAK2) and janus kinase 1 (JAK1) with 20- and 100-fold less in potency respectively. However, in a recent study, the binding affinities (Ki) of tofacitinib citrate towards JAK1, JAK2, and JAK3 were reported to be 1.6 nM, 21.7 nM, and 6.5 nM respectively.

Reference

Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati. Treating inflammation with the janus kinase inhibitor CP-690,550. Trends in Pharmacological Sciences 2011: 32 (1); 25-34