Upadacitinib tartrate tetrahydrate
Based on 27 publication(s) in Google Scholar
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research.
For research use only. We do not sell to patients.
- CAS No.: 1607431-21-9
- Formula: C17H19F3N6O.C4H6O6.4H2O
- Molecular Weight:602.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Upadacitinib tartrate tetrahydrate
More- Cell. 2024 Jan 4;187(1):44-61.e17. [Abstract]
- Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
- Ann Rheum Dis. 2021 Jul;80(7):865-875. [Abstract]
- Nat Commun. 2026 Jan 22;17(1):619. [Abstract]
- Nat Commun. 2025 Jul 29;16(1):6972. [Abstract]
- Nat Commun. 2024 Aug 26;15(1):7165. [Abstract]
- J Adv Res. 2025 Mar 31:S2090-1232(25)00218-8. [Abstract]
- J Control Release. 2024 Jun:370:182-194. [Abstract]
- J Immunother Cancer. 2025 May 11;13(5):e010831. [Abstract]
- Oncogene. 2024 Oct;43(41):3062-3077. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- CNS Neurosci Ther. 2026 Mar;32(3):e70814. [Abstract]
- Life Sci. 2025 Aug 15:375:123698. [Abstract]
- Life Sci. 2025 Aug 15:375:123744. [Abstract]
- Cell Signal. 2025 Jul:131:111706. [Abstract]
- Mol Cell Biochem. 2025 Apr;480(4):2645-2660. [Abstract]
- J Inflamm Res. 2025 Sep 6:18:12295-12309. [Abstract]
- iScience. 2024 Dec 10;28(1):111563. [Abstract]
- ACS Infect Dis. 2023 Dec 8;9(12):2548-2559. [Abstract]
- Biomedicines. 2021 Oct 8;9(10):1413. [Abstract]
- J Neuropathol Exp Neurol. 2025 Jul 23:nlaf085. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2023 Nov 15:1230:123917. [Abstract]
- bioRxiv. 2026 Apr 23.
- bioRxiv. 2025 February 21.
- Patent. US20240216454A1.
- Harvard University. 2024 May.
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ELISA
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Cell Proliferation/Viability Assay
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Flow Cytometry
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RT-PCR
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Flow Cytometry
Biological Activity
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JAK1 0.043 μM (IC50) |
JAK2 0.2 μM (IC50) |
JAK3 2.3 μM (IC50) |
Tyk2 4.7 μM (IC50) |
In biochemical assays, Upadacitinib tartrate tetrahydrate is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance)[1].
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.
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Animal Model:Female Lewis rats (Rat adjuvant-induced arthritis model)[3]
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Dosage:0.1, 0.3, 1, 3, 10 mg/kg
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Administration:Oral gavage; twice a day for 10 days
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Result:Inhibited disease pathology in rat adjuvant induced arthritis.
Chemical Information
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CAS No. 1607431-21-9
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Molecular Weight 602.52
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Formula C17H19F3N6O.C4H6O6.4H2O
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SMILES
O=C(NCC(F)(F)F)N1C[C@H]([C@H](C1)C2=CN=C3C=NC4=C(N32)C=CN4)CC.O=C([C@@H]([C@H](C(O)=O)O)O)O.[4.H2O]
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Synonyms
ABT-494 tartrate tetrahydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (27)
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Journal Impact Factor
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Most Recent
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Cell
2024 Jan 4;187(1):44-61.e17. PMID: 38134932
Upadacitinib tartrate tetrahydrate purchased from MedChemExpress. Usage Cited in: Cell. 2024 Jan 4;187(1):44-61.e17. [Abstract]
Schematic of vehicle (Veh) or Upadacitinib (Upa) (2.5 mg/kg; administered intranasally; twice daily for four consecutive days) treatment of ALT-induced allergic lung inflammation in WT mice. Flow cytometry of lung tissue from vehicle- or upadacitinib-treated mice challenged with intranasal ALT. Shown are the frequencies of ILC2s and eosinophils.
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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
Upadacitinib tartrate tetrahydrate purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
PBLs isolated from healthy participants (n = 6) were pretreated with either vehicle control (0.01% DMSO) or JAK inhibitor Upadacitinib (1 µM, 100 nM, 10 nM) before LPS stimulation. Secreted IL-6 and IL-1β were measured by ELISA 48 hours post-stimulation.
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Ann Rheum Dis
JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib. [Abstract]2021 Jul;80(7):865-875. PMID: 33741556 -
Nat Commun
CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]2026 Jan 22;17(1):619. PMID: 41571637 -
Nat Commun
Autocrine interferon poisoning mediates ADAR1-dependent synthetic lethality in BRCA1/2-mutant cancers. [Abstract]2025 Jul 29;16(1):6972. PMID: 40730818
Upadacitinib tartrate tetrahydrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jul 29;16(1):6972. [Abstract]
Cell survival of SUM149 BRCA1-Mut and BRCA1-Rev cells transfected with a concentration range (nM) of ADAR1 siRNA in the context of exposure to the JAK/STAT pathway inhibitor Upadacitinib ( 32 µM).
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Nat Commun
Type I interferon signaling induces melanoma cell-intrinsic PD-1 and its inhibition antagonizes immune checkpoint blockade. [Abstract]2024 Aug 26;15(1):7165. PMID: 39187481
Upadacitinib tartrate tetrahydrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 26;15(1):7165. [Abstract]
Human melanoma cells pre-incubated with FDA-approved small molecule inhibitors targeting the type I interferon pathway mediators, TYK2 (Deucravacitinib) or JAK1 (Ruxolitinib or Upadacitinib (1 µM)), compared to no IFN-α treatment controls (gray bars), as determined by RT-qPCR and flow cytometry, respectively.
Upadacitinib tartrate tetrahydrate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 26;15(1):7165. [Abstract]
Mouse melanoma cells pre-incubated with FDA-approved small molecule inhibitors targeting the type I interferon pathway mediators, TYK2 (Deucravacitinib) or JAK1 (Ruxolitinib or Upadacitinib (1 µM)), compared to no IFN-α treatment controls (gray bars), as determined by RT-qPCR and flow cytometry, respectively.
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J Adv Res
Metformin attenuates colitis via blocking STAT3 acetylation by reducing acetyl-CoA production. [Abstract]2025 Mar 31:S2090-1232(25)00218-8. PMID: 40174640 -
J Control Release
Can in vitro/in silico tools improve colonic concentration estimations for oral extended-release formulations? A case study with upadacitinib. [Abstract]2024 Jun:370:182-194. PMID: 38641022 -
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 -
Oncogene
RBM12 drives PD-L1-mediated immune evasion in hepatocellular carcinoma by increasing JAK1 mRNA translation. [Abstract]2024 Oct;43(41):3062-3077. PMID: 39187545 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
CNS Neurosci Ther
ShenQi DiHuang Decoction (SQDHD) Ameliorates Neuroinflammation and Neuropsychiatric Manifestations in Pristane Induced Lupus Mice via Blocking JAK1-STAT3 Pathway. [Abstract]2026 Mar;32(3):e70814. PMID: 41795136 -
Life Sci
OASL activates MAPK to drive psoriatic pathogenesis: Astilbin targeting this axis improves metabolic-inflammation crosstalk. [Abstract]2025 Aug 15:375:123698. PMID: 40360089 -
Life Sci
Glucocorticoid reduces mortality in LPS-induced sepsis mouse model by inhibiting JAK1/STAT3-mediated inflammatory response and restoring tricarboxylic acid cycle. [Abstract]2025 Aug 15:375:123744. PMID: 40408938 -
Cell Signal
Paeoniflorin-6'-O-benzene sulfonate inhibits keratinocyte proliferation by restoring GRK2-JAK1 colocalization in mouse model of psoriasis. [Abstract]2025 Jul:131:111706. PMID: 40037425 -
Mol Cell Biochem
Amyloid beta-induced signalling in leptomeningeal cells and its impact on astrocyte response. [Abstract]2025 Apr;480(4):2645-2660. PMID: 39499391 -
J Inflamm Res
Downregulation of IFIT3 Relieves the Inflammatory Response in Ulcerative Colitis via Selectively Regulating Macrophage M1 Polarization and the STAT1/2 Signaling Pathway. [Abstract]2025 Sep 6:18:12295-12309. PMID: 40951449 -
iScience
2024 Dec 10;28(1):111563. PMID: 39868044 -
ACS Infect Dis
Treponema pallidum Promotes the Polarization of M2 Subtype Macrophages to M1 Subtype Mediating the Apoptosis and Inhibiting the Angiogenesis of Human Umbilical Vein Endothelial Cells. [Abstract]2023 Dec 8;9(12):2548-2559. PMID: 37983134 -
Biomedicines
Targeting of Janus Kinases Limits Pro-Inflammatory but Also Immunosuppressive Circuits in the Crosstalk between Synovial Fibroblasts and Lymphocytes. [Abstract]2021 Oct 8;9(10):1413. PMID: 34680530 -
J Neuropathol Exp Neurol
Sodium butyrate improves the effects of brain injury in a small-for-gestational-age rat model by activating the JAK1/STAT3 pathway. [Abstract]2025 Jul 23:nlaf085. PMID: 40700463 -
Mol Pharmacol
Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]2022 Jun;101(6):381-389. PMID: 35383108 -
J Chromatogr B Analyt Technol Biomed Life Sci
Development and validation of a multiplex HPLC-MS/MS assay for the monitoring of JAK inhibitors in patient plasma. [Abstract]2023 Nov 15:1230:123917. PMID: 37956468 -
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Purity & Documentation
References
[1]. Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419. [Content Brief]
[3]. Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018 Aug 28;2:23. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)