Ritlecitinib tosylate
Ritlecitinib, also known as PF-06651600, is a potent and selective JAK3 inhibitor. PF-06651600 is a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies.
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Chemical Information
| Name | Ritlecitinib tosylate |
|---|---|
| Iupac Chemical Name | 1-{(2S,5R)-2-methyl-5-[(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}prop-2-en-1-one tosylate |
| Synonyms | Ritlecitinib tosylate; Ritlecitinib; PF-06651600; PF 06651600; PF06651600; PF-6651600; PF 6651600; PF6651600; |
| Molecular Formula | C22H27N5O4S |
| Molecular Weight | 457.55 |
| Smile | C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=O.OS(=O)(C4=CC=C(C)C=C4)=O |
| InChiKey | YOZLVAFWYLSRRN-VZXYPILPSA-N |
| InChi | InChI=1S/C15H19N5O.C7H8O3S/c1-3-13(21)20-8-11(5-4-10(20)2)19-15-12-6-7-16-14(12)17-9-18-15;1-6-2-4-7(5-3-6)11(8,9)10/h3,6-7,9-11H,1,4-5,8H2,2H3,(H2,16,17,18,19);2-5H,1H3,(H,8,9,10)/t10-,11+;/m0./s1 |
| CAS Number | 2192215-81-7 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message
Sent On: Wed Dec 30 16:23:46 2020
Search: PF-06651600
10 selected items
PubMed Results
Items 1-10 of 10 (Display the 10 citations in PubMed)
1: Robinson MF, Damjanov N, Stamenkovic B, Radunovic G, Kivitz A, Cox L, Manukyan Z, Banfield C, Saunders M, Chandra D, Vincent MS, Mancuso J, Peeva E, Beebe JS. Efficacy and Safety of PF-06651600 (Ritlecitinib), a Novel JAK3/TEC Inhibitor, in Patients With Moderate-to-Severe Rheumatoid Arthritis and an Inadequate Response to Methotrexate. Arthritis Rheumatol. 2020 Oct;72(10):1621-1631. doi: 10.1002/art.41316. Epub 2020 Sep 7. PMID: 32419304; PMCID: PMC7589242.
2: You H, Xu D, Zhao J, Li J, Wang Q, Tian X, Li M, Zeng X. JAK Inhibitors: Prospects in Connective Tissue Diseases. Clin Rev Allergy Immunol. 2020 Dec;59(3):334-351. doi: 10.1007/s12016-020-08786-6. PMID: 32222877.
3: Ismail FF, Sinclair R. JAK inhibition in the treatment of alopecia areata - a promising new dawn? Expert Rev Clin Pharmacol. 2020 Jan;13(1):43-51. doi: 10.1080/17512433.2020.1702878. Epub 2019 Dec 22. PMID: 31865802.
4: Montilla AM, Gómez-García F, Gómez-Arias PJ, Gay-Mimbrera J, Hernández-Parada J, Isla-Tejera B, Ruano J. Scoping Review on the Use of Drugs Targeting JAK/STAT Pathway in Atopic Dermatitis, Vitiligo, and Alopecia Areata. Dermatol Ther (Heidelb). 2019 Dec;9(4):655-683. doi: 10.1007/s13555-019-00329-y. Epub 2019 Oct 13. PMID: 31606872; PMCID: PMC6828894.
5: Xu H, Jesson MI, Seneviratne UI, Lin TH, Sharif MN, Xue L, Nguyen C, Everley RA, Trujillo JI, Johnson DS, Point GR, Thorarensen A, Kilty I, Telliez JB. PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor. ACS Chem Biol. 2019 Jun 21;14(6):1235-1242. doi: 10.1021/acschembio.9b00188. Epub 2019 May 22. PMID: 31082193.
6: D'Amico F, Fiorino G, Furfaro F, Allocca M, Danese S. Janus kinase inhibitors for the treatment of inflammatory bowel diseases: developments from phase I and phase II clinical trials. Expert Opin Investig Drugs. 2018 Jul;27(7):595-599. doi: 10.1080/13543784.2018.1492547. Epub 2018 Jul 6. PMID: 29938545.
7: Robinette ML, Cella M, Telliez JB, Ulland TK, Barrow AD, Capuder K, Gilfillan S, Lin LL, Notarangelo LD, Colonna M. Jak3 deficiency blocks innate lymphoid cell development. Mucosal Immunol. 2018 Jan;11(1):50-60. doi: 10.1038/mi.2017.38. Epub 2017 May 17. PMID: 28513593; PMCID: PMC5693788.
8: Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-y l)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16. PMID: 28139931.
9: Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. doi: 10.1021/acschembio.6b00677. Epub 2016 Nov 10. PMID: 27791347.
10: Walker G, Croasdell G. The European League Against Rheumatism (EULAR) - 17th Annual European Congress of Rheumatology (June 8-11, 2016 - London, UK). Drugs Today (Barc). 2016 Jun;52(6):355-60. doi: 10.1358/dot.2016.52.6.2516435. PMID: 27458612.
Chemical Structure
