Tofacitinib

• UNSPSC Description:

  Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

• Target Antigen:

  Apoptosis; JAK

• Type:

  Reference compound

• Related Pathways:

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

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology; Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Tofacitinib.html

• Purity:

  99.99

• Solubility:

  DMSO : 125 mg/mL (ultrasonic)|Ethanol : 2.5 mg/mL (ultrasonic)

• Smiles:

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

• Molecular Weight:

  312.37

• References & Citations:

  [1]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.|[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]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]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.Acta Pharmacol Sin. 2024 Sep 30.|Ann Rheum Dis. 2021 Sep;80(9):1201-1208.|Ann Rheum Dis. 2024 Aug 20:ard-2024-226067.|Arch Dermatol Res. 2020 Jul;312(5):337-352.|Biochem Pharmacol. 2020 Aug;178:114103.|Biochem Pharmacol. 2023 May 19;213:115618.|Biomed Chromatogr. 2021 Feb 1;e5081.|bioRxiv. 2020 Dec 9;2020.12.09.416586.|bioRxiv. 2024 Jan 24.|bioRxiv. 2024 Oct 23:2024.10.20.619300.|BMC Med. 2021 Oct 15;19(1):247.|Cell Rep Med. 2024 Nov 23:101840.|Cell Rep. 2020 Sep 15;32(11):108158.|Cell Rep. 2024 Oct 11;43(10):114866.|Cell Syst. 2018 Apr 25;6(4):424-443.e7.|Chemrxiv. 2023 Aug 3.|Chemrxiv. Aug 11, 2021.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Exp Cell Res. 2020 Aug 1;393(1):112054.|Exp Cell Res. 2021 Feb 15;399(2):112482.|Food Chem Toxicol. 2020 Dec;146:111835.|Free Radic Biol Med. 2019 Aug 1;139:80-91.|Fundam Clin Pharmacol. 2021 Feb 1.|Inflamm Bowel Dis. 2020 Feb 11;26(3):407-422.|Inflammation. 2023 Jun 13.|Iran J Immunol. 2024 Sep 25;21(3).|iScience. 2021 Sep 25;24(10):103173.|J Allergy Clin Immunol. 2023 Dec 8:S0091-6749(23)02411-9.|J Biochem Mol Toxicol. 2021 Jul 31;e22851.|J Immunol. 2013 Oct 1;191(7):3568-77. |J Pharmacol Exp Ther. 2019 Aug;370(2):137-147. |medRxiv. 2024 Sep 28:2024.09.26.24314341.|Mol Biol Rep. 2022 Dec 12.|Mol Hum Reprod. 2021 Mar 24;27(4):gaab016.|Nano Res. 2023 Apr 15.|Nat Commun. 2024 May 21;15(1):4327.|Patent. US20180263995A1.|Patent. US20220274992A1.|Phytomedicine. November 2022, 154416.|Phytother Res. 2021 Feb;35(2):1033-1047.|PLoS One. 2018 Jan 10;13(1):e0189247. |Pulm Pharmacol Ther. 2017 Apr;43:60-67. |Research Square Preprint. 2024 Apr 19.|Research Square Print. 2022 Aug.|Research Square Print. 2023 Mar 14.|Research Square Print. January 9th, 2023.|Respir Res. 2022 Sep 13;23(1):244.|Sci Adv. 2024 Mar 22;10(12):eadl0368.|Sci Rep. 2021 Apr 1;11(1):7372.|Sci Rep. 2022 May 12;12(1):7843.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Virulence. 2024 Jan 3:2301242.|Cell Mol Gastroenterol Hepatol. 2021 Oct 6;S2352-345X(21)00192-2.|Cell Prolif. 2021 Jan;54(1):e12933.|Eur J Pharm Sci. 2024 Jul 4:106845.|Int J Rheum Dis. 2020 Aug;23(8):1066-1075.|J Med Chem. 2021 Feb 11.|Pharmaceuticals. 2024 Jan 8, 17(1), 77.|Stem Cell Res Ther. 2024 Jun 18;15(1):177.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Launched

• CAS Number:

  477600-75-2