Ritlecitinib malonate
Based on 9 publication(s) in Google Scholar
Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).
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- CAS No.: 2140301-97-7
- Formule: C18H23N5O5
- Masse moléculaire:389.41
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) Ritlecitinib malonate
More- Ann Rheum Dis. 2025 Sep 25:S0003-4967(25)04383-3. [Abstract]
- Blood Adv. 2022 Jul 26;6(14):4283-4296. [Abstract]
- Int J Mol Sci. 2024 Dec 15;25(24):13452. [Abstract]
- Int J Mol Sci. 2023 May 25;24(11):9243. [Abstract]
- Expert Opin Investig Drugs. 2021 Dec;30(12):1169-1174. [Abstract]
- Clin Immunol. 2025 Apr:273:110445. [Abstract]
- Res Sq. 2026 Apr 13.
- bioRxiv. 2026 Mar 7.
- bioRxiv. 2023 Aug 17.
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RT-PCR
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Activité biologique
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JAK3 33.1 nM (IC50) |
IL-2 |
IL-4 |
IL7R |
IL-15 |
STAT3 |
STAT5 |
STAT6 |
Ritlecitinib malonate inhibits IL-15 in peripheral blood mononuclear cells (PBMCs) and heparin treated human whole blood (HWB) with IC50 of 51 nM and 197 nM, respectively[1].
Ritlecitinib malonate inhibits the phosphorylation of STAT proteins mediated by IL-2 (STAT5), IL-4 (STAT6), IL-7 (STAT5), IL-15 (STAT5), and IL-21 (STAT3) at concentrations of 244 nM, 340 nM, 407 nM, 266 nM, and 355 nM (IC50), respectively[2].
Ritlecitinib malonate (30 nM, 167 nM; 5 days, 6 days) inhibits cell differentiation in Th1 and Th17 cell differentiation inhibition experiments for 5 days under Th1 conditions and 6 days under Th17 conditions, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse splenocytes, human whole blood lymphocytes (HWB)
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Concentration:33.1 nM, 244 nM, 340 nM, 407 nM, 266 nM, 355 nM
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Incubation Time:1 hour (pre-treatment with Ritlecitinib malonate) + 15-20 minutes (cytokine stimulation)
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Result:In mouse splenocytes, 33.1 nM inhibited JAK3 kinase activity, while 244 nM, 340 nM, 407 nM, and 266 nM inhibited STAT5 phosphorylation induced by IL-2, IL-4, IL-7, and IL-15 respectively. In human whole blood lymphocytes, 355 nM inhibited IL-21-induced STAT3 phosphorylation.
Ritlecitinib (30, 100 mg/kg (reversal); 20, 60 mg/kg (prevention); oral; once daily) malonate reduces disease severity in the mouse experimental autoimmune encephalomyelitis (EAE) model[2].
Ritlecitinib (30 mg/kg; oral; once daily; 4 weeks) malonate can prevent the occurrence of alopecia areata in the C3H/HeJ mouse skin transplantation alopecia areata prevention model; Ritlecitinib (30 mg/kg; oral; once daily; 12 weeks) malonate can reverse the symptoms of alopecia areata, promote hair regeneration and reduce skin inflammation in the C3H/HeJ mouse alopecia areata model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeJ mice (8-week-old) with alopecia areata model[3]
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Dosage:30 mg/kg Ritlecitinib
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Administration:Oral via ALZET osmotic pump; once daily; 12 weeks
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Result:Significantly induced hair regrowth, reduced skin-infiltrating CD45+ leukocytes, CD44+CD62L−CD8+ T cells, NKG2D+CD8+ T cells, and IFN-γ+CD8+ T cells, and decreased Alopecia areata (AA)-associated skin inflammation.
Chemical Information
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CAS No. 2140301-97-7
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Masse moléculaire 389.41
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Formule C18H23N5O5
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SMILES
OC(CC(O)=O)=O.C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O
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Synonyms
PF-06651600 malonate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (9)
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Journal Impact Factor
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Most Recent
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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 -
Blood Adv
Latent membrane proteins from EBV differentially target cellular pathways to accelerate MYC-induced lymphomagenesis. [Abstract]2022 Jul 26;6(14):4283-4296. PMID: 35605249 -
Int J Mol Sci
Epstein-Barr Virus BRRF1 Induces Butyrophilin 2A1 in Nasopharyngeal Carcinoma NPC43 Cells via the IL-22/JAK3-STAT3 Pathway. [Abstract]2024 Dec 15;25(24):13452. PMID: 39769218
Ritlecitinib malonate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Dec 15;25(24):13452. [Abstract]
Ritlecitinib (0.5-5 μM) significantly decreased the gene expression level of BTN2A1 in NPC43 cells.
Ritlecitinib malonate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Dec 15;25(24):13452. [Abstract]
STAT3, p-STAT3, STAT1, p-STAT1, STAT5, p-STAT5, JNK, and p-JNK protein expression of NPC43 cells by BRRF1 overexpression with or without Ritlecitinib (5 μM) treatment. Representative immunoblots are shown.
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Int J Mol Sci
JAK Signaling Is Critically Important in Cytokine-Induced Viral Susceptibility of Keratinocytes. [Abstract]2023 May 25;24(11):9243. PMID: 37298195 -
Expert Opin Investig Drugs
Ritlecitinib: an investigational drug for the treatment of moderate to severe alopecia areata. [Abstract]2021 Dec;30(12):1169-1174. PMID: 34826225 -
Clin Immunol
Novel janus kinase 3 inhibitor ritlecitinib suppresses T and B cell responses to prevent acute cardiac allograft rejection in mice. [Abstract]2025 Apr:273:110445. PMID: 39954912 -
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Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ritlecitinib malonate Related Classifications
HY-100754A Related Classifications
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