An internal standard for the quantification of tofacitinib
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Unlabeled Version(s)
11598Tofacitinib (citrate)
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Tofacitinib-d3 (citrate)

Item No. 25046

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R,4R)-4-methyl-3-(methyl-d3-7H-pyrrolo[2,3-d]pyrimidin-4R-ylamino)-β-oxo-1-piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate
Synonyms
  • CP 690,550-d3
Molecular Formula
C16H17D3N6O • C6H8O7
Formula Weight
507.5
Purity
≥99% deuterated forms (d1-d3)
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleWater: soluble
SMILES
O=C(CC#N)N1CC[C@@H](C)[C@@H](N(C([2H])([2H])[2H])C2=NC=NC3=C2C=CN3)C1.OC(CC(O)=O)(C(O)=O)CC(O)=O
InChi Code
InChI=1S/C16H20N6O.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t11-,13+;/m1./s1/i2D3;
InChi Key
SYIKUFDOYJFGBQ-OGNQCBPOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $735

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    Product Description

    Tofacitinib-d3 (citrate) is intended for use as an internal standard for the quantification of tofacitinib (Item No. 11598) by GC- or LC-MS. Tofacitinib is a potent, cell-permeable inhibitor of all JAK isoforms (IC50s = 6.1, 12, and 8 nM for JAK1, JAK2, and JAK3, respectively).1 It is selective for JAK1-3 over ROCK-2 and Lck (IC50s = 3,400 and 3,870 nM, respectively) as well as 28 additional kinases in enzyme assays (IC50s = >10,000 nM). It inhibits IL-2-mediated phosphorylation of JAK3 and STAT5 when used at a concentration of 30 ng/ml.2 Tofacitinib prevents rejection and prolongs survival in murine and cynomolgus monkey models of heterotopic heart and kidney transplantation, respectively. Formulations containing tofacitinib have been used in the prevention of organ allograft rejection as well as in the treatment of the inflammatory or autoimmune components of a host of diseases, including rheumatoid arthritis and ulcerative colitis.2,3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Haan, C., Rolvering, C., Raulf, F., et al. Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors. Chem. Biol. 18(3), 314-323 (2011).

    2. Changelian, P.S., Flanagan, M.E., Ball, D.J., et al. Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor. Science 302(5646), 875-878 (2003).

    3. Flanagan, M.E., Blumenkopf, T.A., Brissette, W.H., 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. J. Med. Chem. 53(24), 8468-8484 (2010).

    4. Cutolo, M. The kinase inhibitor tofacitinib in patients with rheumatoid arthritis: Latest findings and clinical potential. Ther. Adv. Musculoskelet. Dis. 5(1), 3-11 (2013).

    5. Sandborn, W.J., Ghosh, S., Panes, J., et al. Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis. N. Engl. J. Med. 367(7), 616-624 (2012).