Tofacitinib-d3 (citrate)

• UNSPSC Description:

  Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

• Target Antigen:

  Apoptosis; Bacterial; Fungal; Influenza Virus; Isotope-Labeled Compounds; JAK

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Anti-infection;Apoptosis;Epigenetics;JAK/STAT Signaling;Others;Protein Tyrosine Kinase/RTK;Stem Cell/Wnt

• Applications:

  COVID-19-anti-virus

• Field of Research:

  Cancer; Infection; Inflammation/Immunology

• Purity:

  99.14

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(CC#N)N1C[C@H](N(C2=C3C(NC=C3)=NC=N2)C([2H])([2H])[2H])[C@H](C)CC1.O=C(CC(C(O)=O)(O)CC(O)=O)O

• Molecular Weight:

  507.51

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.|[2]Jiang JK, et al. Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J Med Chem. 2008 Dec 25;51(24):8012-8.|[3]LaBranche TP, et al. JAK inhibition with tofacitinib suppresses arthritic joint structural damage through decreased RANKL production. Arthritis Rheum. 2012 Nov;64(11):3531-42.|[4]Onda M, et al. Tofacitinib suppresses antibody responses to protein therapeutics in murine hosts. J Immunol. 2014 Jul 1;193(1):48-55.|[5]Yagi K, et al. Pharmacological inhibition of JAK3 enhances the antitumor activity of STI571 in human chronic myeloid leukemia. Eur J Pharmacol. 2018 Apr 15;825:28-33.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  No Development Reported

• CAS Number:

  2701680-77-3