Tofacitinib citrate Inhibitor CAS No. 540737-29-9

Product Name	Tofacitinib citrate
Synonyms	CP-690550 citrate
CAS No.	540737-29-9
Molecular Weight	504.49
Formula	C₁₆H₂₀N₆O.C₆H₈O₇
Chemical Name	3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile citrate
Smiles	N1(C[C@@H]([C@@H](CC1)C)N(c1c2c(ncn1)[nH]cc2)C)C(=O)CC#N C(C(CC(=O)O)(C(=O)O)O)C(=O)O
Chemical Structure
Documents	HPLC MS COA

Biological activities

Tofacitinib citrate is a PAN-JAK inhibitor with phenomenal selectivity against the human kinome. Tofacitinib citrate inhibits JAK3 activity with an IC50 of 1 nM. The binding affinities (K_{i) of tofacitinib citrate for JAK1, JAK2 and JAK3 are 1.6, 21.7, 6.5 nM, respectively, while the comparable binding affinities (Kd) for JAK3 and JAK2 are 5 and 2.2 nM, respectively. Meanwhile, tofacitinib citrate significantly reduces NK cell numbers by nearly 80%, CD8+ T cell numbers by almost 43%, respectively. ^[1] In vitro, tofacitinib citrate potently inhibits IL-4 induced upregulation of CD23 with an IC50 of 57 nM and class II major histocompatibility complex (MHCII) expression with an IC50 of 71 nM. ^[2] Tofacitinib citrate also significantly reduces 80% BAL eosinophil numbers when administered during ovalbumin challenge. In addition, BAL levels of IL-13 and eotaxin are reduced by tofacitinib citrate in 79% and 97%, respectively. ^[3] Tofacitinib citrate exerts greater antiproliferative and proapoptotic activity against cells harboring JAK2^V617F compared with JAK2^WT, with IC50s of 0.25 and 2.1 µM, respectively. At the same time, tofacitinib citrate treatment of ex-vivo-expanded erythroid progenitors from JAK2^V617F-positive PV patients resulted in a specific, antiproliferative IC50 of 0.2 µM and proapoptotic activity.^[4] Animals dosed with tofacitinib citrate (15 mg/kg/d) during the period of antigen sensitization and boost demonstrated marked reductions in BAL eosinophils and levels of IL-13 and eotaxin following ovalbumin aerosol exposure.^[3] Receiving a combination of tofacitinib citrate and MMF, Anemia and gastroin-testinal (GI) disturbances are observed with a weight loss of 8.5% in animals. ^[1]}

Protocols

Tofacitinib citrate is stored as a 10 mM stock solution in DMSO at ??0°C. ^[4]

References

[1] Lalitha V, et al. Treating inflammation with the Janus Kinase inhibitor CP-690550. Trends in Pharmacol Sci. 2011, 32: 26-33. [2] Elizabeth K, et al. The JAK-3 inhibitor CP-690550 is a potent anti- inflammatory agent in a murine model of pulmonary eosinophilia. Eur J of Pharmacol. 2008, 582:154-161. [3] Fumie K, et al. Therapeutic effect of IL-12/23 and their signaling pathway blockade on brain ischemia model. Biochem and Biophys Res Commun. 2010, 402: 500-506. [4] Taghi M, et al. The JAK kinase inhibitor CP-690550 supresses the growth of human polycythemia vera cells carrying the JAK2V617F mutation. Cancer Sci. 2008, 99: 1265-1273.

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