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Tofacitinib-d3 (citrate) (Synonyms: CP 690,550-d3)

Catalog No.GC49692

An internal standard for the quantification of tofacitinib

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Tofacitinib-d3 (citrate) Chemical Structure

Cas No.: N/A

Taille Prix Stock Qté
1 mg
942,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Tofacitinib-d3 (citrate) is intended for use as an internal standard for the quantification of tofacitinib 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

1.Haan, C., Rolvering, C., Raulf, F., et al.Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptorsChem. 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 inhibitorScience302(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 rejectionJ. Med. Chem.53(24)8468-8484(2010) 4.Cutolo, M.The kinase inhibitor tofacitinib in patients with rheumatoid arthritis: Latest findings and clinical potentialTher. 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 colitisN. Engl. J. Med.367(7)616-624(2012)

Chemical Properties

Cas No. N/A SDF Download SDF
Synonymes CP 690,550-d3
Canonical 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
Formula C16H17D3N6O • C6H8O7 M.Wt 507.5
Solubility DMSO: soluble,Water: soluble Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9704 mL 9.8522 mL 19.7044 mL
5 mM 0.3941 mL 1.9704 mL 3.9409 mL
10 mM 0.197 mL 0.9852 mL 1.9704 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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