Tofacitinib citrate
Based on 94 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 540737-29-9
- Formula: C22H28N6O8
- Molecular Weight:504.49
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
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Biological Activity
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Publications Citing Use of MedChemExpress (MCE) Tofacitinib citrate
More- Nature. 2025 Jun;642(8066):201-211. [Abstract]
- Adv Mater. 2025 Dec 12:e13952. [Abstract]
- Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
- Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]
- Ann Rheum Dis. 2021 Sep;80(9):1201-1208. [Abstract]
- Nat Commun. 2026 May 11. [Abstract]
- Nat Commun. 2025 Sep 29;16(1):8560. [Abstract]
- Nat Commun. 2024 May 21;15(1):4327. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Adv Sci (Weinh). 2024 Dec 5:e2410360. [Abstract]
- Adv Sci (Weinh). 2024 Dec 11:e2407398. [Abstract]
- Sci Adv. 2024 Mar 22;10(12):eadl0368. [Abstract]
- J Allergy Clin Immunol. 2024 Apr;153(4):1125-1139. [Abstract]
- Gut Microbes. 2025 Dec;17(1):2526136. [Abstract]
- MedComm (2020). 2025 Jun 6;6(6):e70212. [Abstract]
- J Immunother Cancer. 2025 May 11;13(5):e010831. [Abstract]
- J Immunother Cancer. 2025 Apr 8;13(4):e010783. [Abstract]
- Cell Rep Med. 2024 Nov 23:101840. [Abstract]
- Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2426660122. [Abstract]
- Nano Res. 2023 Apr 15.
- Acta Pharmacol Sin. 2025 Feb;46(2):353-365. [Abstract]
- Phytomedicine. 2025 Sep 23:148:157326. [Abstract]
- Phytomedicine. 2022 Nov:106:154416. [Abstract]
- BMC Med. 2021 Oct 15;19(1):247. [Abstract]
- Free Radic Biol Med. 2026 Mar 16:246:334-349. [Abstract]
- Free Radic Biol Med. 2019 Aug 1:139:80-91. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2025;19(5):101447. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2022;13(2):383-404. [Abstract]
- Stem Cell Res Ther. 2024 Jun 18;15(1):177. [Abstract]
- Cell Rep. 2024 Oct 11;43(10):114866. [Abstract]
- Cell Rep. 2020 Sep 15;32(11):108158. [Abstract]
- J Med Chem. 2021 Feb 25;64(4):2228-2241. [Abstract]
- Phytother Res. 2021 Feb;35(2):1033-1047. [Abstract]
- Biochem Pharmacol. 2025 Dec 2:244:117586. [Abstract]
- Biochem Pharmacol. 2023 Jul:213:115618. [Abstract]
- Cell Prolif. 2021 Jan;54(1):e12933. [Abstract]
- Biochem Pharmacol. 2020 Aug;178:114103. [Abstract]
- Virulence. 2024 Dec;15(1):2301242. [Abstract]
- Drug Des Devel Ther. 2025 Jun 10:19:5043-5057. [Abstract]
- Inflammation. 2023 Oct;46(5):1764-1776. [Abstract]
- Respir Res. 2022 Sep 13;23(1):244. [Abstract]
- Pharmaceuticals (Basel). 2024 Jan 8;17(1):77. [Abstract]
- Eur J Pharm Sci. 2026 Jan 1:216:107365. [Abstract]
- Eur J Pharm Sci. 2024 Jul 4:106845. [Abstract]
- Rheumatology (Oxford). 2025 Aug 13:keaf437. [Abstract]
- Inflamm Bowel Dis. 2020 Feb 11;26(3):407-422. [Abstract]
- iScience. 2024 Dec 10;28(1):111563. [Abstract]
- iScience. 2021 Sep 25;24(10):103173. [Abstract]
- J Biomed Mater Res A. 2026 Feb;114(2):e70035. [Abstract]
- J Biotechnol. 2025 Mar:399:9-18. [Abstract]
- Sci Rep. 2022 May 12;12(1):7843. [Abstract]
- Sci Rep. 2021 Apr 1;11(1):7372. [Abstract]
- Food Sci Nutr. 2026 Mar 4;14(3):e71602. [Abstract]
- J Pharmacol Exp Ther. 2019 Aug;370(2):137-147. [Abstract]
- Mol Hum Reprod. 2021 Mar 24;27(4):gaab016. [Abstract]
- Exp Cell Res. 2021 Feb 15;399(2):112482. [Abstract]
- Food Chem Toxicol. 2020 Dec;146:111835. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- J Immunol. 2013 Oct 1;191(7):3568-77. [Abstract]
- Mol Biol Rep. 2023 Feb;50(2):1477-1485. [Abstract]
- J Biochem Mol Toxicol. 2021 Sep;35(9):e22851. [Abstract]
- Pulm Pharmacol Ther. 2017 Apr:43:60-67. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2018 Jan 10;13(1):e0189247. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- Immunobiology. 2025 Nov;230(6):153136. [Abstract]
- Arch Dermatol Res. 2020 Jul;312(5):337-352. [Abstract]
- Planta Med. 2025 Oct 20. [Abstract]
- Int J Rheum Dis. 2020 Aug;23(8):1066-1075. [Abstract]
- Biomed Chromatogr. 2021 Jun;35(6):e5081. [Abstract]
- Iran J Immunol. 2024 Sep 25;21(3). [Abstract]
- bioRxiv. 2026 May 29.
- bioRxiv. 2026 May 5.
- J Can Res Updates. 2026.
- bioRxiv. 2026 Feb 11:2026.02.10.704860. [Abstract]
- SSRN. 2025 Sep 3.
- Res Sq. 2025 Sep 26.
- bioRxiv. 2025 Aug 16.
- Res Sq. 2025 Apr 16.
- bioRxiv. 2025 February 21.
- medRxiv. 2024 Sep 28:2024.09.26.24314341. [Abstract]
- bioRxiv. 2024 Oct 23:2024.10.20.619300. [Abstract]
- Research Square Preprint. 2024 Apr 19.
- bioRxiv. 2024 Jan 24.
- Chemrxiv. 2023 Aug 3.
- Research Square Print. 2023 Mar 14.
- Research Square Print. January 9th, 2023.
- Patent. US20220274992A1.
- Research Square Print. 2022 Aug.
- Chemrxiv. Aug 11, 2021.
- bioRxiv. 2020 Dec 9:2020.12.09.416586. [Abstract]
- Patent. US20180263995A1.
Customer Validation & Images
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Flow Cytometry
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Flow Cytometry
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Cell Imaging/Staining
Biological Activity
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JAK3 1 nM (IC50) |
JAK2 20 nM (IC50) |
JAK1 112 nM (IC50) |
Rock-II 3400 nM (IC50) |
Lck 3870 nM (IC50) |
Tofacitinib (CP-690550) citrate binds potentially at JAK3 and JAK2 as 2.2 nM and 5 nM (Kd). The report includes additional binding for Tofacitinib at Camk1 (Kd of 5,000 nM), DCamkL3 (Kd of 4.5 nM), Mst2 (Kd of 4,300 nM), Pkn1 (Kd of 200 nM), Rps6ka2 (Kin.Dom.2-C-terminal) (Kd of 1,400 nM), Rps6ka6 (Kin.Dom.2-C-terminal) (Kd of 1,200 nM), Snark (Kd of 420 nM), Tnk1 (Kd of 640 nM) and Tyk2 (Kd of 620 nM)[1].
K562, KCL22, and THP-1 cells are exposed to different doses of STI571 or JAK inhibitors for 72 h to quantify the effects of tyrosine kinase inhibitor (TKI) activity. Cell growth inhibition is then evaluated using the MTT assay. The proliferation of K562 and KCL22 cells, but not THP-1 cells, is inhibited by IMA in a concentration-dependent manner. The IC50 value of IMA is 0.28 μM for K562 and 0.17 μM for KCL22. Although treatment with Tofacitinib (TOF) or INCB018424 alone does not suppress cell proliferation, both Tofacitinib and INCB018424 make the K562 and KCL22 more sensitive to IMA[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 540737-29-9
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Appearance Solid
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Molecular Weight 504.49
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Formula C22H28N6O8
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Color White to off-white
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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
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Synonyms
Tasocitinib citrate; CP-690550 citrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
Publications (94)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jun;642(8066):201-211. PMID: 40269158 -
Adv Mater
3D Bioprinted Human Synovium-Cartilage Models Mimic Rheumatoid Arthritis Microenvironment and Recapitulate In Vivo Therapeutic Responses. [Abstract]2025 Dec 12:e13952. PMID: 41388589 -
Ann Rheum Dis
Augmentation of immunothrombosis as a key mechanism underlying JAK inhibition associated hypercoagulability in rheumatoid arthritis. [Abstract]2025 Sep 25:S0003-4967(25)04383-3. PMID: 41006174 -
Ann Rheum Dis
2024 Aug 20:ard-2024-226067. PMID: 39164066
Tofacitinib citrate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]
Western blot analysis was performed to detect PU.1 expression in Jurkat and EL4 cells treated with recombinant IL-9 and the JAK inhibitor tofacitinib (10 μM, 48 h).
Tofacitinib citrate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]
Western blot analysis was performed to detect the IL-9 effect on the JAK1/STAT3 pathway in RA-Th9 cells. The cell treated with tofacitinib (10 μM, 48 h), stattic (2.5 μM, 48 h).
Tofacitinib citrate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]
Flow cytometry was used to detect the JAK inhibitor tofacitinib (10 μM, 48 h) effect, STAT3 inhibitor stattics (2.5 μM, 48 h), and PU.1 inhibitor DB2313 on the release of IL-9 from Th9 cells.
Tofacitinib citrate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]
Flow cytometry was used to detect IL-9 and JAK inhibitor tofacitinib (10 μM, 48 h) effect, STAT3 inhibitor stattics (2.5 μM, 48 h) effect on TNF-α-induced apoptosis in Th9 cells.
Tofacitinib citrate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2024 Aug 20:ard-2024-226067. [Abstract]
Assess the effects of tofacitinib (10 μM, 48 h), stattics (2.5 μM, 48 h), and IL-9mAb on the cell migration of RA-FLS after treatment with the supernatant from RA-Th9 cells.
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Ann Rheum Dis
Immune response to dermatomyositis-specific autoantigen, transcriptional intermediary factor 1γ can result in experimental myositis. [Abstract]2021 Sep;80(9):1201-1208. PMID: 33811031 -
Nat Commun
All-trans retinoic acid destabilizes ADAR1 protein through retinoylation-mediated USP7 dissociation and improves immunotherapy in pancreatic cancer. [Abstract]2026 May 11. PMID: 42115161 -
Nat Commun
A loss-of-function human ADAR variant activates innate immune response and promotes bowel inflammation. [Abstract]2025 Sep 29;16(1):8560. PMID: 41022715 -
Nat Commun
Priming with LSD1 inhibitors promotes the persistence and antitumor effect of adoptively transferred T cells. [Abstract]2024 May 21;15(1):4327. PMID: 38773088 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]2024 Dec 5:e2410360. PMID: 39639496 -
Adv Sci (Weinh)
MAM-STAT3-Driven Mitochondrial Ca+2 Upregulation Contributes to Immunosenescence in Type A Mandibuloacral Dysplasia Patients. [Abstract]2024 Dec 11:e2407398. PMID: 39661729 -
Sci Adv
2024 Mar 22;10(12):eadl0368. PMID: 38507500 -
J Allergy Clin Immunol
Recapitulating primary immunodeficiencies with expanded potential stem cells: proof-of-concept with STAT1 gain-of-function. [Abstract]2024 Apr;153(4):1125-1139. PMID: 38072195 -
Gut Microbes
The PTPN2 rs1893217 IBD risk allele increases susceptibility to AIEC invasion by a JAK-STAT-CEACAM6 axis. [Abstract]2025 Dec;17(1):2526136. PMID: 40624731 -
MedComm (2020)
Loss of Adenosine Deaminase Acting on RNA 1 Induces Panoptosis and Immune Response in Ulcerative Colitis Gut Mucosa. [Abstract]2025 Jun 6;6(6):e70212. PMID: 40487746 -
J Immunother Cancer
Combinatorial treatment with upadacitinib abrogates systemic toxicity of a tumor-targeted IL-2 fusion protein. [Abstract]2025 May 11;13(5):e010831. PMID: 40350206 -
J Immunother Cancer
JAK3 A573V and JAK3 M511I mutations in peripheral T-cell lymphoma mediating resistance to anti-PD-1 therapy through the STAT3/PD-L1 pathway. [Abstract]2025 Apr 8;13(4):e010783. PMID: 40199606 -
Cell Rep Med
Chemical activation of mitochondrial ClpP to modulate energy metabolism of CD4+ T cell for inflammatory bowel diseases treatment. [Abstract]2024 Nov 23:101840. PMID: 39626672 -
Proc Natl Acad Sci U S A
2025 Jun 17;122(24):e2426660122. PMID: 40489618 -
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Acta Pharmacol Sin
Tofacitinib prevents depressive-like behaviors through decreased hippocampal microgliosis and increased BDNF levels in both LPS-induced and CSDS-induced mice. [Abstract]2025 Feb;46(2):353-365. PMID: 39349767 -
Phytomedicine
Astragali radix - Curcumae rhizoma herb pair enhances Sorafenib's efficacy by inducing ferroptosis and activates Th1 cell immune response synergistically against hepatocellular carcinoma. [Abstract]2025 Sep 23:148:157326. PMID: 41016296 -
Phytomedicine
Anemoside B4 protects against chronic relapsing colitis in mice by modulating inflammatory response, colonic transcriptome and the gut microbiota. [Abstract]2022 Nov:106:154416. PMID: 36037770 -
BMC Med
HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]2021 Oct 15;19(1):247. PMID: 34649530 -
Free Radic Biol Med
Inhibiting Arachidonate-5-lipoxygenase expression ameliorates osteoarthritis progression by suppressing ferroptosis via the JAK2/STAT3 signaling pathway. [Abstract]2026 Mar 16:246:334-349. PMID: 41581577 -
Free Radic Biol Med
Oxidative stress-induced IL-15 trans-presentation in keratinocytes contributes to CD8+ T cells activation via JAK-STAT pathway in vitiligo. [Abstract]2019 Aug 1:139:80-91. PMID: 31078730 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Cell Mol Gastroenterol Hepatol
Tofacitinib Mitigates the Increased SARS-CoV-2 Infection Susceptibility Caused by an IBD Risk Variant in the PTPN2 Gene. [Abstract]2025;19(5):101447. PMID: 39756517 -
Cell Mol Gastroenterol Hepatol
Tofacitinib-Induced Modulation of Intestinal Adaptive and Innate Immunity and Factors Driving Cellular and Systemic Pharmacokinetics. [Abstract]2022;13(2):383-404. PMID: 34624526 -
Stem Cell Res Ther
LncRNA SNHG1 enhances cartilage regeneration by modulating chondrogenic differentiation and angiogenesis potentials of JBMMSCs via mitochondrial function regulation. [Abstract]2024 Jun 18;15(1):177. PMID: 38886785 -
Cell Rep
2024 Oct 11;43(10):114866. PMID: 39395168 -
Cell Rep
The Natural Compound Notopterol Binds and Targets JAK2/3 to Ameliorate Inflammation and Arthritis. [Abstract]2020 Sep 15;32(11):108158. PMID: 32937124 -
J Med Chem
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof. [Abstract]2021 Feb 25;64(4):2228-2241. PMID: 33570945 -
Phytother Res
Paeoniflorin-6'-o-benzene sulfonate (CP-25) improves vasculitis through inhibiting IL-17A/JAK/STAT3 signaling pathway in endothelial cells of HFD CIA rats. [Abstract]2021 Feb;35(2):1033-1047. PMID: 33006176 -
Biochem Pharmacol
Glucocorticoid impairs angiogenesis-dependent osteogenesis by downregulating EphB4 in endothelial cells. [Abstract]2025 Dec 2:244:117586. PMID: 41344513 -
Biochem Pharmacol
2023 Jul:213:115618. PMID: 37211172 -
Cell Prolif
FGF9 promotes mouse spermatogonial stem cell proliferation mediated by p38 MAPK signalling. [Abstract]2021 Jan;54(1):e12933. PMID: 33107118 -
Biochem Pharmacol
Combined anti-fibrotic and anti-inflammatory properties of JAK-inhibitors on macrophages in vitro and in vivo: Perspectives for scleroderma-associated interstitial lung disease. [Abstract]2020 Aug;178:114103. PMID: 32562787 -
Virulence
Immunosuppressants exert antiviral effects against influenza A(H1N1)pdm09 virus via inhibition on nucleic acid synthesis, mRNA splicing and protein stability. [Abstract]2024 Dec;15(1):2301242. PMID: 38170681 -
Drug Des Devel Ther
Drug Interaction Potential of Berberine Hydrochloride When Co-Administered with Tofacitinib and Filgotinib in Rats. [Abstract]2025 Jun 10:19:5043-5057. PMID: 40524804 -
Inflammation
2023 Oct;46(5):1764-1776. PMID: 37310645 -
Respir Res
IL-37 protects against airway remodeling by reversing bronchial epithelial-mesenchymal transition via IL-24 signaling pathway in chronic asthma. [Abstract]2022 Sep 13;23(1):244. PMID: 36100847 -
Pharmaceuticals (Basel)
Topical Delivery of Tofacitinib in Dermatology: The Promise of a Novel Therapeutic Class Using Biodegradable Dendritic Polyglycerol Sulfates. [Abstract]2024 Jan 8;17(1):77. PMID: 38256910 -
Eur J Pharm Sci
Assessing the effects of tofacitinib on the gut microbiome in inflammatory bowel disease. [Abstract]2026 Jan 1:216:107365. PMID: 41205933 -
Eur J Pharm Sci
Exploring the interactions of JAK inhibitor and S1P receptor modulator drugs with the human gut microbiome: Implications for colonic drug delivery and inflammatory bowel disease. [Abstract]2024 Jul 4:106845. PMID: 38971433 -
Rheumatology (Oxford)
Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]2025 Aug 13:keaf437. PMID: 40802538 -
Inflamm Bowel Dis
The JAK-Inhibitor Tofacitinib Rescues Human Intestinal Epithelial Cells and Colonoids from Cytokine-Induced Barrier Dysfunction. [Abstract]2020 Feb 11;26(3):407-422. PMID: 31751457 -
iScience
2024 Dec 10;28(1):111563. PMID: 39868044 -
iScience
Schlafen 11 expression in human acute leukemia cells with gain-of-function mutations in the interferon-JAK signaling pathway. [Abstract]2021 Sep 25;24(10):103173. PMID: 34693224 -
J Biomed Mater Res A
A ROS-Responsive Hydrogel Microneedle System Co-Delivering Tofacitinib and Azelaic Acid for Enhanced Targeted Therapy of Rosacea. [Abstract]2026 Feb;114(2):e70035. PMID: 41586451 -
J Biotechnol
2025 Mar:399:9-18. PMID: 39824361 -
Sci Rep
Identification of novel off targets of baricitinib and tofacitinib by machine learning with a focus on thrombosis and viral infection. [Abstract]2022 May 12;12(1):7843. PMID: 35551258 -
Sci Rep
JAK/STAT inhibitor therapy partially rescues the lipodystrophic autoimmune phenotype in Clec16a KO mice. [Abstract]2021 Apr 1;11(1):7372. PMID: 33795715 -
Food Sci Nutr
Chlorogenic Acid Ameliorate Lipopolysaccharide Induced Intestinal Acute Inflammatory Injury via Inhibiting Cytokines Production and Activating Intestinal Stem Cells. [Abstract]2026 Mar 4;14(3):e71602. PMID: 41788896 -
J Pharmacol Exp Ther
Novel Inhaled Pan-JAK Inhibitor, LAS194046, Reduces Allergen-Induced Airway Inflammation, Late Asthmatic Response, and pSTAT Activation in Brown Norway Rats. [Abstract]2019 Aug;370(2):137-147. PMID: 31085698 -
Mol Hum Reprod
2021 Mar 24;27(4):gaab016. PMID: 33693775 -
Exp Cell Res
Down-regulation of A3AR signaling by IL-6-induced GRK2 activation contributes to Th17 cell differentiation. [Abstract]2021 Feb 15;399(2):112482. PMID: 33434531 -
Food Chem Toxicol
Gallic and butyric acids modulated NLRP3 inflammasome markers in a co-culture model of intestinal inflammation. [Abstract]2020 Dec;146:111835. PMID: 33130239 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
J Immunol
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. [Abstract]2013 Oct 1;191(7):3568-77. PMID: 24006460 -
Mol Biol Rep
Janus kinase inhibitor Tofacitinib alleviated acute hepatitis induced by lipopolysaccharide/D-galactosamine in mice. [Abstract]2023 Feb;50(2):1477-1485. PMID: 36507969 -
J Biochem Mol Toxicol
Lung-derived exosomes regulate the function of mesenchymal stem cells and alleviate phosgene-induced lung injury via miR-34c-3p. [Abstract]2021 Sep;35(9):e22851. PMID: 34331784 -
Pulm Pharmacol Ther
Tofacitinib ameliorates inflammation in a rat model of airway neutrophilia induced by inhaled LPS. [Abstract]2017 Apr:43:60-67. PMID: 28087469
Tofacitinib citrate purchased from MedChemExpress. Usage Cited in: Pulm Pharmacol Ther. 2017 Apr:43:60-67. [Abstract]
Effect of Tofacitinib administered 1 h before LPS challenge. (A) Effect of different doses of Tofacitinib on STAT3 activation in lung homogenates obtained 30 min after LPS challenge. (B) Effect of different doses of Tofacitinib on STAT3 activation in lung homogenates obtained 4 h after LPS challenge.
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PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
Application of a phenotypic drug discovery strategy to identify biological and chemical starting points for inhibition of TSLP production in lung epithelial cells. [Abstract]2018 Jan 10;13(1):e0189247. PMID: 29320511 -
Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
Immunobiology
Dual-phase study of CD4+CXCR4+ T cells in Mycoplasma pneumoniae pneumonia: clinical correlations in children and therapeutic exploration with tofacitinib in mice. [Abstract]2025 Nov;230(6):153136. PMID: 41192098 -
Arch Dermatol Res
2020 Jul;312(5):337-352. PMID: 31786711 -
Planta Med
Active Components and Multi-target Mechanism of Tibetan Sinopodophyllum hexandrum Medicine Against Rheumatoid Arthritis Using a CFA-induced Arthritis Rat Model. [Abstract]2025 Oct 20. PMID: 41115426 -
Int J Rheum Dis
MiR-1193 represses the proliferation and induces the apoptosis of interleukin-1β-treated fibroblast-like synoviocytes via targeting JAK3. [Abstract]2020 Aug;23(8):1066-1075. PMID: 32597556 -
Biomed Chromatogr
Identification of the metabolites of tofacitinib in liver microsomes by liquid chromatography combined with high resolution mass spectrometry. [Abstract]2021 Jun;35(6):e5081. PMID: 33522621 -
Iran J Immunol
2024 Sep 25;21(3). PMID: 39319693 -
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bioRxiv
Multiplexed high-content imaging uncovers morphological diversity of lymphocyte activation and dysfunction. [Abstract]2026 Feb 11:2026.02.10.704860. PMID: 41726991 -
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medRxiv
The JAK inhibitor, Tofacitinib, Corrects the Overexpression of CEACAM6 and Limits Susceptibility to AIEC Caused by Reduced Activity of the IBD Associated Gene, PTPN2. [Abstract]2024 Sep 28:2024.09.26.24314341. PMID: 39399045 -
bioRxiv
All-trans retinoic acid-mediated ADAR1 degradation synergizes with PD-1 blockade to suppress pancreatic cancer. [Abstract]2024 Oct 23:2024.10.20.619300. PMID: 39484589 -
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bioRxiv
Identification of a Novel Susceptibility Marker for SARS-CoV-2 Infection in Human Subjects and Risk Mitigation with a Clinically Approved JAK Inhibitor in Human/Mouse Cells. [Abstract]2020 Dec 9:2020.12.09.416586. PMID: 33330862 -
Solvent & Solubility
DMSO : 41.67 mg/mL (82.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 3.33 mg/mL (6.60 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cell survival assay is performed using MTT. Briefly, K562, KCL22, and THP-1 cells (1×105 cells/well) are plated onto 96-well microplates and treated with or without IMA (0.06-1.0 μM) and/or Tofacitinib (10-1,000 nM) or RUX (10-1,000 nM) for 72 h at 37°C in a humidified 5% (v/v) CO2 atmosphere. The medium (200 µL) is then incubated with 10 µL of 5 mg/ml MTT solution for 4 h at 37°C. After being centrifuged at 352 g for 5 min, the culture medium is removed, and 100 µL of DMSO are added to each well to dissolve the formazan. Absorbance is measured at 570 nm using a microplate reader. The results are expressed as percentages[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Female BALB/c mice (6-8 weeks old) are used. Mice receive Tofacitinib in PEG300 (100 mg/mL) or vehicle alone (PEG300) by osmotic pump infusion (0.25 μL/hour, 28 days). Four days prior to immunization, mice are anesthetized and their dorsal surface is shaved. A one cm incision is made on the back to create a subcutaneous pocket and insert the pump. The incision site is closed with wound clips. Mice are injected weekly (i.p.) with SS1P recombinant immunotoxin (RIT; 5 μg/mouse) beginning on day 0; control mice received injections of saline alone. Every week before SS1P or vehicle immunization, 50 μL of blood is drawn to obtain serum samples. Sera are stored at -80°C until analyzed.
Rats[3]
Adjuvant-induced arthritis (AIA) is induced in female Lewis rats. Rats are randomized according to hind paw volume and assigned to Tofacitinib or vehicle treatment regimens. Groups of 7-8 rats per treatment group, and normal naive rats (n=4 per group), are euthanized either 4 hours, 4 days, or 7 days after beginning treatment (days 16, 20, and 23 after immunization, respectively). Once-daily oral administration of vehicle or Tofacitinib (6.2 mg/kg) is initiated on day 16 following immunization and continued through day 23. Paw volumes are reassessed 4 and 7 days after the beginning of treatment (days 20 and 23 after immunization, respectively). For micro-computed tomography (micro-CT) imaging, as well as tartrate-resistant acid phosphatase (TRAP) staining in paw tissue, AIA is induced in a separate cohort of Lewis rats.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Onda M, et al. Tofacitinib suppresses antibody responses to protein therapeutics in murine hosts. J Immunol. 2014 Jul 1;193(1):48-55. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9822 mL | 9.9110 mL | 19.8220 mL | 49.5550 mL |
| 5 mM | 0.3964 mL | 1.9822 mL | 3.9644 mL | 9.9110 mL | |
| DMSO | 10 mM | 0.1982 mL | 0.9911 mL | 1.9822 mL | 4.9555 mL |
| 15 mM | 0.1321 mL | 0.6607 mL | 1.3215 mL | 3.3037 mL | |
| 20 mM | 0.0991 mL | 0.4955 mL | 0.9911 mL | 2.4777 mL | |
| 25 mM | 0.0793 mL | 0.3964 mL | 0.7929 mL | 1.9822 mL | |
| 30 mM | 0.0661 mL | 0.3304 mL | 0.6607 mL | 1.6518 mL | |
| 40 mM | 0.0496 mL | 0.2478 mL | 0.4955 mL | 1.2389 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9911 mL | |
| 60 mM | 0.0330 mL | 0.1652 mL | 0.3304 mL | 0.8259 mL | |
| 80 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6194 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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