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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

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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

Description Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.
Targets JAK3          
IC50 1 nM          

Protocol

Cell experiment [1]:

Cell lines

Naïve T cell

Preparation method

This product is soluble in DMSO mostly at 198 mM. It is also soluble in water with no more than 1 mM.

Reacting condition

16h; 50 nM

Applications

A concentration of 100 nM. 50 nM, but not 10 nM, CP-690,550 suppressed IFN- c production 4 days after Th1 differentiation conditions were established, while both 10 nM and 50 nM CP-690,550 strongly suppressed IL-4 production under Th2 differentiation conditions. This suggests that CP-690,550 inhibits both Th1 and Th2 differentiation, and that Th2 is more sensitive than Th1 to this drug. We then examined the effect of CP-690,550 on Th17 and induced T regulatory (iTreg) cells. CP-690,550 enhanced IL-17 production while suppressing Foxp3 and IL-10 induction in a dose-dependent manner under Th17 differentiation conditions. These data indicate that <100 nM CP-690,550 efficiently inhibits Th1, Th2 and iTreg while promoting Th17, in vitro.

Animal experiment [1]:

Animal models

C57BL6/J mice and DBA/1J mice

Dosage form

30 nM; intraperitoneal injection

Application

Naïve CD4+T cells isolated from mice were stimulated with various cytokines in the presence of various concentrations of CP-690,550. CP-690,550 selectively inhibited IFN c -induced STAT1, IL-4-induced STAT6, and IL-2-induced STAT5 at 3–30 nM, while 30 nM CP-690,550 did not suppress IL-6-induced STAT3 phosphorylation. A concentration greater than 100 nM was required for the partial suppression of STAT3

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Yoshida H, Kimura A, Fukaya T, et al. Low dose CP-690,550 (tofacitinib), a pan-JAK inhibitor, accelerates the onset of experimental autoimmune encephalomyelitis by potentiating Th17 differentiation[J]. Biochemical and biophysical research communications, 2012, 418(2): 234-240.

intraperitoneal injection

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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