Tofacitinib (citrate)
Tofacitinib citrate is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
Product Specifications
CAS Number
[540737-29-9]
Product Name Alternative
Tasocitinib (citrate) ; CP-690550 (citrate)
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; Bacterial; Fungal; Influenza Virus; JAK
Type
Reference compound
Related Pathways
Anti-infection; Apoptosis; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
COVID-19-anti-virus
Field of Research
Cancer; Infection; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/Tofacitinib-citrate.html
Purity
99.94
Solubility
DMSO : 41.67 mg/mL (ultrasonic) |H2O : 3.33 mg/mL (ultrasonic)
Smiles
O=C(CC#N)N1C[C@H](N(C2=C3C(NC=C3)=NC=N2)C)[C@H](C)CC1.O=C(CC(C(O)=O)(O)CC(O)=O)O
Molecular Formula
C22H28N6O8
Molecular Weight
504.49
Precautions
H302, H315, H319, H335
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]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 and light)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
JAK1; JAK2; JAK3
Citation 01
Cell Mol Gastroenterol Hepatol. 2022;13 (2) :383-404.|Cell Prolif. 2021 Jan;54 (1) :e12933.|Eur J Pharm Sci. 2024 Jul 4:106845.|Eur J Pharm Sci. 2025 Nov 6;216:107365.|Int J Rheum Dis. 2020 Aug;23 (8) :1066-1075.|J Med Chem. 2021 Feb 25;64 (4) :2228-2241.|Pharmaceuticals (Basel) . 2024 Jan 8;17 (1) :77.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|Stem Cell Res Ther. 2024 Jun 18;15 (1) :177.|Acta Pharmacol Sin. 2025 Feb;46 (2) :353-365.|Adv Sci (Weinh) . 2024 Dec 11:e2407398.|Adv Sci (Weinh) . 2024 Dec 5:e2410360.|Ann Rheum Dis. 2021 Sep;80 (9) :1201-1208.|Ann Rheum Dis. 2024 Aug 20:ard-2024-226067.|Ann Rheum Dis. 2025 Sep 25:S0003-4967 (25) 04383-3.|Arch Dermatol Res. 2020 Jul;312 (5) :337-352.|Biochem Pharmacol. 2020 Aug;178:114103.|Biochem Pharmacol. 2023 Jul:213:115618.|Biomed Chromatogr. 2021 Jun;35 (6) :e5081.|bioRxiv. 2020 Dec 9:2020.12.09.416586.|bioRxiv. 2024 Jan 24.|bioRxiv. 2024 Oct 23:2024.10.20.619300.|bioRxiv. 2025 Aug 16.|bioRxiv. 2025 February 21.|BMC Med. 2021 Oct 15;19 (1) :247.|Cell Mol Gastroenterol Hepatol. 2025.|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.|Drug Des Devel Ther. 2025 Jun 10:19:5043-5057.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|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 Oct;35 (5) :919-929.|Gut Microbes. 2025 Dec;17 (1) :2526136.|Immunobiology. 2025 Nov;230 (6) :153136.|Inflamm Bowel Dis. 2020 Feb 11;26 (3) :407-422.|Inflammation. 2023 Oct;46 (5) :1764-1776.|Iran J Immunol. 2024 Sep 25;21 (3) .|iScience. 2021 Sep 25;24 (10) :103173.|iScience. 2024 Dec 10;28 (1) :111563.|J Allergy Clin Immunol. 2024 Apr;153 (4) :1125-1139.|J Biochem Mol Toxicol. 2021 Sep;35 (9) :e22851.|J Biotechnol. 2025 Mar:399:9-18.|J Immunol. 2013 Oct 1;191 (7) :3568-77. |J Immunother Cancer. 2025 Apr 8;13 (4) :e010783.|J Immunother Cancer. 2025 May 11;13 (5) :e010831.|J Pharmacol Exp Ther. 2019 Aug;370 (2) :137-147.|MedComm (2020) . 2025 Jun 6;6 (6) :e70212.|medRxiv. 2024 Sep 28:2024.09.26.24314341.|Mol Biol Rep. 2023 Feb;50 (2) :1477-1485.|Mol Hum Reprod. 2021 Mar 24;27 (4) :gaab016.|Nano Res. 2023 Apr 15.|Nat Commun. 2024 May 21;15 (1) :4327.|Nat Commun. 2025 Sep 29;16 (1) :8560.|Nature. 2025 Jun;642 (8066) :201-211.|Patent. US20180263995A1.|Patent. US20220274992A1.|Phytomedicine. 2022 Nov:106:154416.|Phytomedicine. 2025 Sep 23:148:157326.|Phytother Res. 2021 Feb;35 (2) :1033-1047.|Planta Med. 2025 Oct 20.|PLoS One. 2018 Jan 10;13 (1) :e0189247. |Proc Natl Acad Sci U S A. 2025 Jun 17;122 (24) :e2426660122.|Pulm Pharmacol Ther. 2017 Apr:43:60-67.|Res Sq. 2025 Apr 16.|Res Sq. 2025 Sep 26.|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.|Rheumatology (Oxford) . 2025 Aug 13:keaf437.|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.|SSRN. 2025 Sep 3.|Virulence. 2024 Dec;15 (1) :2301242.
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