Cat. No.: HY-40354A

Tofacitinib citrate

Name: Tofacitinib citrate
Brand: MedChemExpress
SKU: HY-40354A
Price: 42.00 USD
Availability: InStock
Rating: 5 (103 reviews)

(Synonyms: Tasocitinib citrate; CP-690550 citrate)

103 Cited Publications

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Based on 103 publication(s) in Google Scholar

Tofacitinib citrate (Tasocitinib citrate) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib citrate blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib citrate can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

For research use only. We do not sell to patients.

Purity: 99.94%
CAS No.: 540737-29-9
Formula: C₂₂H₂₈N₆O₈
Molecular Weight:504.49

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)

Tofacitinib citrate Chemical Structure

CAS No.: 540737-29-9

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (103)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
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Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]^[9]

JAK1

JAK3

STAT1

NF-κB

STAT6

STAT3

All JAK Isoforms :

All STAT Isoforms :

All NF-κB Isoforms :

In Vitro

Tofacitinib (1000 nM; 3 days) citrate (Tasocitinib citrate) suppresses proliferation and Th17 cell differentiation of SKG mouse spleen CD4⁺ T cells in vitro^[2].
Tofacitinib (5 days) citrate suppresses differentiation of naïve SKG mouse lung-infiltrating cells into CD11b⁺ Gr1_dim and CD11b⁺ CD11c⁺ cells, while increasing CD11b_dim CD11c⁺ cell proportions in vitro^[2].
Tofacitinib (5 days) citrate facilitates expansion of MDSCs and suppresses BMDC differentiation from naïve SKG mouse bone marrow cells in vitro^[2].
Tofacitinib (1 μM; 60 min) citrate abrogates IL6-induced STAT3 phosphorylation and reduces fibrotic marker expression in neonatal foreskin primary fibroblasts^[4].
Tofacitinib (2 μM; 24 h) citrate alters gene expression in white adipocytes, generating a distinct Tofacitinib gene signature^[4].
Tofacitinib (1 μM; 24 hr pre-incubation) citrate inhibits IL-4-induced JAK/STAT6 signaling in primary murine bone marrow macrophages, but does not provide sustained inhibitory activity after a 72 hr washout period^[5].
Tofacitinib citrate selectively inhibits Janus kinases 1, Janus kinases 2, and Janus kinases 3 with functional specificity for Janus kinases 1 and Janus kinases 3 over Janus kinase 2, and suppresses cytokine-mediated immune cell activation and pro-inflammatory signaling in vitro^[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[5]

Cell Line:

primary murine bone marrow macrophages
Concentration:

1 μM
Incubation Time:

24 hr pre-incubation
Result:

Inhibited the JAK/STAT6 signaling pathway induced by IL-4 in primary mouse bone marrow macrophages, but could not maintain its inhibitory activity after 72 hours of elution.

In Vivo

Tofacitinib (10-75 mg/kg; i.g.; daily; 1 week) citrate (Tasocitinib citrate) alleviates LPS-induced depressive-like behaviors and associated hippocampal pathological changes, with 30 mg/kg showing robust efficacy in reducing microgliosis, normalizing cytokine levels, and restoring BDNF levels^[1].
Tofacitinib (30 mg/kg; i.g.; daily; 13 days) citrate effectively improves depressive-like behaviors, including social avoidance, in CSDS-induced mice^[1].
Tofacitinib (10-75 mg/kg; i.g.; daily; 1 week) citrate is well-tolerated and does not affect emotional status in normal mice^[1].
Tofacitinib (30 mg/kg; i.p.; twice daily; 5 days/week; 5 weeks) citrate reduces established skin fibrosis in male TSK1/+ mice on a C57BL/6 background^[4].
Tofacitinib (20 mg/kg; i.p.; three times per week; 8 weeks) citrate ameliorates zymosan-induced interstitial lung disease in male SKG mice by increasing lung MDSCs to 72.8% of total lung cells and reducing pathogenic Th17 cells, ILC1s, and GM-CSF⁺ ILCs^[2].
Tofacitinib (1-10 mg/kg; i.g.; every 6 hours starting 2 hours post-CLP) citrate improves the 7-day survival rate of CLP-induced septic rats to 70%, reduces acute lung injury, and inhibits the JAK-STAT/NF-κB pathway^[3].
Tofacitinib (10 mg/kg; p.o.; daily; 8 weeks) citrate prevents murine lupus manifestations, modulates innate and adaptive immune responses, improves vascular function, and restores lipoprotein homeostasis in lupus-prone MRL/lpr mice^[8].
Tofacitinib (10 mg/kg; p.o.; daily; 6 weeks) citrate ameliorates established murine lupus manifestations and modulates interferon responses in lupus-prone MRL/lpr mice^[8].
Tofacitinib (10 mg/kg/day; i.g.; every 2 days; 2 weeks) citrate relieves liver fibrosis in a mouse model of chronic autoimmune hepatitis^[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (10-week-old male, LPS-induced depressive-like behavior)^[1]
Dosage:

10 mg/kg; 30 mg/kg; 75 mg/kg
Administration:

i.g.; daily; 1 week
Result:

Showed a protective effect on LPS-induced weight loss in a dose-dependent manner at 10 mg/kg and 30 mg/kg, while the effect of 75 mg/kg on body weight was limited.
Showed a tendency for improvement in depressive-like behaviors at 10 mg/kg, and significantly attenuated depressive-like behaviors (reduced immobility time in forced swim and tail suspension tests) at 30 mg/kg and 75 mg/kg.
Did not alter locomotor activity in the open field test.
Reversed the LPS-induced increased phosphorylation of JAK3, STAT1, and STAT3 in the hippocampus at 30 mg/kg.
Significantly decreased JAK/STAT-mediated cytokine (CCL2, IL-1β, TNF-α) transcription and microgliosis in the hippocampus, and restored LPS-reduced BDNF mRNA and protein levels in the hippocampus at 30 mg/kg.

Animal Model:

C57BL/6 (6-week-old male, CSDS-induced depressive-like behavior)^[1]
Dosage:

30 mg/kg
Administration:

i.g.; daily; 13 days
Result:

Significantly increased social interaction (social index and time in interaction zone) in CSDS-induced mice, with no effect on body weight.
Showed reduced immobility time in the forced swim test and tail suspension test, and increased locomotor activity in the open field test compared to untreated CSDS-induced mice.

Animal Model:

C57BL/6 (10-week-old male)^[1]
Dosage:

10 mg/kg; 30 mg/kg; 75 mg/kg
Administration:

i.g.; daily; 1 week
Result:

Did not significantly alter body weight, locomotor activity, or emotional behaviors in naïve mice.

Animal Model:

SKG mice (male, 8-9 weeks old, zymosan-induced interstitial lung disease)^[2]
Dosage:

20 mg/kg
Administration:

i.p.; three times per week; 8 weeks
Result:

Suppressed progression of interstitial lung disease, reducing the lung histological score relative to control.
Increased the proportion of myeloid-derived suppressor cells (MDSCs) to 72.8% of total lung cells.
Decreased the proportion of RORγt+ CD4+ Th17 cells.
Decreased the number of T-bet+ group 1 innate lymphoid cells (ILC1s).
Decreased the number of GM-CSF+ ILCs.
Suppressed phosphorylation of STAT1 and STAT5 (but not STAT3) in lung MDSCs.

Animal Model:

Sprague-Dawley (male, 8-10 weeks old, 250-300 g, CLP-induced sepsis model)^[3]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

i.g.; every 6 hours starting 2 hours post-CLP
Result:

Increased 7-day survival rate to 40%.
Increased 7-day survival rate to 50%.
Increased 7-day survival rate to 70%.
Reduced lung histopathological damage scores.
Decreased lung wet/dry weight ratio.
Inhibited lung tissue expression of IL-6, TNF-α, IL-1β, and IFN-γ.
Reduced CLP-induced increases in phosphorylated STAT3 and phosphorylated NF-κB protein levels in lung tissue.

Animal Model:

TSK1/+ mice (C57BL/6 background; 5-week-old male; non-inflammatory skin fibrosis model)^[4]
Dosage:

30 mg/kg
Administration:

i.p.; twice daily; 5 days/week; 5 weeks
Result:

Significantly attenuated hypodermal thickening.
Reduced phosphorylated STAT3-positive cell counts in skin.

Animal Model:

MRL/MpJ-Faslpr/lpr/J (MRL/lpr) (female, 10 weeks old, spontaneous lupus-prone model)^[8]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 8 weeks
Result:

Blocked the appearance of anti-nuclear antibodies (ANA) and anti-dsDNA antibodies.
Reduced glomerulonephritis histopathologic scores, immune complex deposition in kidneys, and urine albumin:creatinine ratio.
Reduced skin inflammation and hyperplasia.
Decreased spleen size and total splenocyte counts.
Reduced total T cell, CD8+ T cell, and double-negative (DN) CD3+CD4−CD8− T cell counts.
Normalized serum levels of pro-inflammatory cytokines including TNF-α, IFN-γ, IL-17A, IL-2, and MIP1-α (CCL3).
Reduced expression of interferon-stimulated genes (ISGs) including Mx1, CXCL10, Isg15, IFIT1, STAT1, and STAT2 in splenocytes and kidney tissue.
Decreased spontaneous and LPS-induced neutrophil extracellular trap (NET) release.
Improved endothelium-dependent vasorelaxation.
Increased the capacity of endothelial progenitor cells (EPCs) to differentiate into mature endothelial cells.
Increased total HDL cholesterol and HDL cholesteryl ester levels.
Reduced red blood cell counts, hemoglobin concentration, and hematocrit.

Animal Model:

MRL/MpJ-Faslpr/lpr/J (MRL/lpr) (female, 14 weeks old, spontaneous lupus-prone model with established active disease)^[8]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 6 weeks
Result:

Reduced anti-dsDNA antibody levels.
Decreased urine albumin:creatinine ratio.
Reduced serum blood urea nitrogen (BUN) and creatinine levels.
Increased the capacity of endothelial progenitor cells (EPCs) to differentiate into mature endothelial cells.
Reduced expression of interferon-stimulated genes (ISGs) including Mx1, CXCL10, STAT1, Isg15, and IFIT1.

Animal Model:

C57BL/6 (male, 6-8 weeks old, 18-20 g, chronic immune-mediated hepatitis with liver fibrosis induced by initial intravenous adenovirus injection followed by repeated hydrodynamic tail vein transfection with pCYP2D6 plasmid)^[9]
Dosage:

10 mg/kg/day
Administration:

i.g.; every 2 days; 2 weeks
Result:

Alleviated liver fibrosis in mice with autoimmune hepatitis, as evidenced by reduced Sirius red staining of liver tissue.

Chemical Information

CAS No. 540737-29-9
Appearance Solid
Molecular Weight 504.49
Formula C₂₂H₂₈N₆O₈
Color White to off-white
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
Synonyms

Tasocitinib citrate; CP-690550 citrate
Shipping

Room temperature in continental US; may vary elsewhere.
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 (103)

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Nature

Microbial metabolite drives ageing-related clonal haematopoiesis via ALPK1. [Abstract]

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

Positive feedback loop PU.1-IL9 in Th9 promotes rheumatoid arthritis development. [Abstract]

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.
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
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
Adv Sci (Weinh)

MAM-STAT3-Driven Mitochondrial Ca+2 Upregulation Contributes to Immunosenescence in Type A Mandibuloacral Dysplasia Patients. [Abstract]

2025 Feb;12(5):e2407398. PMID: 39661729
Adv Sci (Weinh)

Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]

2025 Jan;12(4):e2410360. PMID: 39639496
Cell Rep Med

Chemical activation of mitochondrial ClpP to modulate energy metabolism of CD4+ T cell for inflammatory bowel diseases treatment. [Abstract]

2024 Dec 17;5(12):101840. PMID: 39626672
Sci Adv

JAK/STAT signaling pathway affects CCR5 expression in human CD4+ T cells. [Abstract]

2024 Mar 22;10(12):eadl0368. PMID: 38507500
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
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
Phytomedicine

2026 Oct:160:158639. PMID: 42537464
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
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
Proc Natl Acad Sci U S A

PARP12-mediated mono-ADP-ribosylation as a checkpoint for necroptosis and apoptosis. [Abstract]

2025 Jun 17;122(24):e2426660122. PMID: 40489618
Nano Res

2023 Apr 15.
Dev Cell

Tumor-intrinsic FDFT1 determines coordinated macrophage anti-tumor immunity. [Abstract]

2026 Apr 29:S1534-5807(26)00150-4. PMID: 42061405
BMC Med

HBeAg mediates inflammatory functions of macrophages by TLR2 contributing to hepatic fibrosis. [Abstract]

2021 Oct 15;19(1):247. PMID: 34649530
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
Phytother Res

(+)-Matairesinol, Derived From Olive Oil, Enhanced T-Cell Anti-Tumor Immune via JAK3-STAT1 Signal and Synergized With Anti-PD-1 Efficacy. [Abstract]

2026 Apr 27. PMID: 42037203
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
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
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

IL-33/TGF-β/IL-4-induced bone marrow-derived DC9 subset promotes Th9 differentiation and allergic airway inflammation. [Abstract]

2026 Jun 4;45(6):117519. PMID: 42247295
Cell Rep

LTP expression mediated by autonomous activity of GluN2B-bound CaMKII. [Abstract]

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
Cell Prolif

FGF9 promotes mouse spermatogonial stem cell proliferation mediated by p38 MAPK signalling. [Abstract]

2021 Jan;54(1):e12933. PMID: 33107118
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
J Med Chem

Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof. [Abstract]

2021 Feb 25;64(4):2228-2241. PMID: 33570945
J Ethnopharmacol

"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]

2026 Oct 28:369:121888. PMID: 42202911
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
CNS Neurosci Ther

Hypoxia Upregulates RIPK1 via the HIF-1α-JAK-STAT Pathway Leading to Astrocyte Necroptosis to Promote Cavitation After Spinal Cord Injury. [Abstract]

2026 May;32(5):e70895. PMID: 42109032
Biochem Pharmacol

Glucocorticoid impairs angiogenesis-dependent osteogenesis by downregulating EphB4 in endothelial cells. [Abstract]

2026 Feb:244:117586. PMID: 41344513
Biochem Pharmacol

STING activation in macrophages by vanillic acid exhibits antineoplastic potential. [Abstract]

2023 Jul:213:115618. PMID: 37211172
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
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
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
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
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
Inflammation

The Effect of JAK Inhibitor Tofacitinib on Chondrocyte Autophagy. [Abstract]

2023 Oct;46(5):1764-1776. PMID: 37310645
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 Sep 1:200:106845. PMID: 38971433
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
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
Rheumatology (Oxford)

Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]

2025 Aug 13:keaf437. PMID: 40802538
iScience

IFN-γ licenses normal and pathogenic ALPK1/TIFA pathway in human monocytes. [Abstract]

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
Pain Rep

2026 Jul 10;11(4):e1475. PMID: 42444784
FASEB J

Targeting JAK2: Genetic and Pharmacological Inhibition Attenuates Immune-Mediated Liver Injury by Suppressing Proinflammatory Macrophage. [Abstract]

2026 Apr 30;40(8):e71804. PMID: 41984049
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

Tofacitinib alters STAT3 signaling and leads to endometriosis lesion regression. [Abstract]

2021 Mar 24;27(4):gaab016. PMID: 33693775
J Biotechnol

Interferon inhibitors increase rAAV production in HEK293 cells. [Abstract]

2025 Mar:399:9-18. PMID: 39824361
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
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
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.
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
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
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
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
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
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
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

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Arch Dermatol Res

Effect of propylene glycol on the skin penetration of drugs. [Abstract]

2020 Jul;312(5):337-352. PMID: 31786711
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
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

2026 Jul;29(7):e70773. PMID: 42453001
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

JAK/STAT Signaling Pathway Mediates Anti-Tumor Immunity of CD8+ T Cells in Renal Cancer. [Abstract]

2024 Sep 25;21(3). PMID: 39319693
bioRxiv

2026 May 29.
bioRxiv

2026 May 5.
J Can Res Updates

2026.
bioRxiv

Multiplexed high-content imaging uncovers morphological diversity of lymphocyte activation and dysfunction. [Abstract]

2026 Feb 11:2026.02.10.704860. PMID: 41726991
Res Sq

2025 Sep 26.
SSRN

2025 Sep 3.
bioRxiv

2025 Aug 16.
Res Sq

2025 Apr 16.
bioRxiv

2025 February 21.
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
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
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

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
Patent

US20180263995A1.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9822 mL

9.9110 mL

19.8220 mL

5 mM

0.3964 mL

1.9822 mL

3.9644 mL

10 mM

0.1982 mL

0.9911 mL

1.9822 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.43 mg/mL (2.83 mM); Clear solution

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 2.5 mg/mL (4.96 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (312 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gao YN, et al. Tofacitinib prevents depressive-like behaviors through decreased hippocampal microgliosis and increased BDNF levels in both LPS-induced and CSDS-induced mice. Acta pharmacologica Sinica. 2025 Feb;46(2):353-365. [Content Brief]

[2]. Sendo S, et al. Tofacitinib facilitates the expansion of myeloid-derived suppressor cells and ameliorates interstitial lung disease in SKG mice. Arthritis research & therapy. 2019 Aug 06;21(1):184.

[3]. Zhang X, et al. Tofacitinib reduces acute lung injury and improves survival in a rat model of sepsis by inhibiting the JAK-STAT/NF-κB pathway. Journal of inflammation (London, England). 2023 Feb 03;20(1):5.

[4]. Wang W, et al. The JAK/STAT pathway is activated in systemic sclerosis and is effectively targeted by tofacitinib. Journal of scleroderma and related disorders. 2020 Feb;5(1):40-50.

[5]. Wei X, et al. Development of a Janus Kinase Inhibitor Prodrug for the Treatment of Rheumatoid Arthritis. Molecular pharmaceutics. 2018 Aug 06;15(8):3456-3467.

[6]. Fleischmann R, et al. Placebo-controlled trial of tofacitinib monotherapy in rheumatoid arthritis. N Engl J Med. 2012 Aug 9;367(6):495-507.

[7]. Sandborn WJ, et al. Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis. N Engl J Med. 2012 Aug 16;367(7):616-24.

[8]. Furumoto Y, et al. Tofacitinib Ameliorates Murine Lupus and Its Associated Vascular Dysfunction. Arthritis & rheumatology (Hoboken, N.J.). 2017 Jan;69(1):148-160.

[9]. Wang H, et al. The JAK inhibitor tofacitinib ameliorates immune‑mediated liver injury in mice. Molecular medicine reports. 2019 Dec;20(6):4883-4892.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
H₂O / DMSO	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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Tofacitinib citrate

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Tofacitinib citrate

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All JAK Isoforms

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All NF-κB Isoforms