Tofacitinib-13C3,15N

Tofacitinib-13C3,15N (Tasocitinib-13C3,15N) is 13C and 15N labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

Tasocitinib-13C3,15N; CP-690550-13C3,15N

12352005

Apoptosis; Isotope-Labeled Compounds; JAK

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

COVID-19-immunoregulation

Inflammation/Immunology; Cancer

O=[13C]([13CH2][13C]#C)N1C[C@H](N(C2=C3C(NC=C3)=NC=N2)C)[C@H](C)CC1.[15N]

C14 13C3H21N5 15NO

329.36

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Onda M, et al. Tofacitinib suppresses antibody responses to protein therapeutics in murine hosts. J Immunol. 2014 Jul 1;193 (1) :48-55.|[3]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.|[4]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.|[5]Calama E, et al. Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS. Pulm Pharmacol Ther. 2017 Apr;43:60-67.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-40354S1/

Isotope-Labeled Compounds

No Development Reported