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Tofacitinib (CP-690550) Citrate

Tofacitinib (CP-690550) Citrate

Catalog Number:
L002369044APE
Mfr. No.:
APE-A4135
Price:
$196
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      • Overview

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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.

      • Properties
        • Alternative Name
          Tasocitinib citrate,CP 690550 citrate; 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
          CAS Number
          540737-29-9
          Molecular Formula
          C16H20N6O·C6H8O7
          Molecular Weight
          504.49
          Appearance
          A solid
          Purity
          98.82%
          Solubility
          ≥25.22 mg/mL in DMSO; insoluble in EtOH; ≥3.4 mg/mL in H2O with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference

        • 1. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID:31862381
          2. McInnes IB, Byers NL, et al. "Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations." Arthritis Res Ther. 2019 Aug 2;21(1):183. PMID:31375130
          3. Liu S, Verma M, et al. "Steroid resistance of airway type 2 innate lymphoid cells from patients with severe asthma: The role of thymic stromal lymphopoietin."J Allergy Clin Immunol. 2018 Jan;141(1):257-268.e6. PMID:28433687
          4. Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID:25701119

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