477600-75-2
477600-75-2
Chemical Structure
Tofacitinib
Synonym(s): Tasocitinib; CP-690550
- CAS. Nr.: 477600-75-2
- Formula:C16H20N6O
- Molecular Weight:312.37
IUPAC Name: 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile
InChIKey: UJLAWZDWDVHWOW-YPMHNXCESA-N
SMILES: O=C(CC#N)N1C[C@H](N(C2=C3C(NC=C3)=NC=N2)C)[C@H](C)CC1
Biological Activity: Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury[1][2][3][4][5][6][7][8][9].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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Tofacitinib | 99.94% | Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | ||||||||||||||||||||
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Tofacitinib (Standard) | 99.96% | Tofacitinib (Standard) (Tasocitinib (Standard); CP-690550 (Standard)) is the analytical standard of Tofacitinib (HY-40354). This product is intended for research and analytical applications. Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | ||||||||||||||||||||
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Tofacitinib-13C | Tofacitinib-13C (Tasocitinib-13C; CP-690550-13C) is the 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | |||||||||||||||||||||
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Tofacitinib-13C,d3 | Tofacitinib-13C,d3 (Tasocitinib-13C,d3; CP-690550-13C,d3) is the deuterated, 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | |||||||||||||||||||||
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Tofacitinib-d3 | Tofacitinib-d3 (Tasocitinib-d3; CP-690550-d3) is the deuterated-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | |||||||||||||||||||||
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Tofacitinib-13C3,15N | 99.57% | Tofacitinib-13C3,15N (Tasocitinib-13C3,15N; CP-690550-13C3,15N) is the 15N, 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | ||||||||||||||||||||
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Tofacitinib-13C3 | 99.77% | Tofacitinib-13C3 (Tasocitinib-13C3; CP-690550-13C3) is the 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury. | ||||||||||||||||||||
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CP-690550A | CP-690550A is an analogue of Tofacitinib (HY-40354). CP-690550A is a dual inhibitor of JAK2 and JAK3. | |||||||||||||||||||||
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Tofacitinib impurity 6 | Tofacitinib impurity 6 is an impurity of Tofacitinib (HY-40354). | |||||||||||||||||||||
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N-Methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine dihydrochloride | 99.86% | N-Methyl-N-((3R,4R)-4-methylpiperidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine dihydrochloride is a drug intermediate for synthesis of various active compounds. | ||||||||||||||||||||
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(3S,4R)-Tofacitinib | 99.80% | (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM. | ||||||||||||||||||||
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(3S,4S)-Tofacitinib | 99.28% | (3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM. | ||||||||||||||||||||
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(3R,4S)-Tofacitinib | 99.74% | (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM. | ||||||||||||||||||||
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Tofacitinib Impurity T | 99.80% | Tofacitinib Impurity T (3-((3R,4R)-4-Methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanamide) is a drug intermediate for synthesis of various active compounds. | ||||||||||||||||||||
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Tofacitinib impurity 3 | 99.84% | Tofacitinib impurity 3 is an impurity of Tofacitinib (HY-40354). | ||||||||||||||||||||
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Tofacitinib impurity 32 | 99.53% | Tofacitinib impurity 32 is an impurity of Tofacitinib (HY-40354). | ||||||||||||||||||||
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Tofacitinib impurity 32 (Standard) | ≥98% | 1-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)ethanone (Standard) is the analytical standard of 1-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)ethanone. This product is intended for research and analytical applications. | ||||||||||||||||||||
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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.
