Ritlecitinib tosylate | CAS#2192215-81-7 | JAK3 inhibitor

MedKoo Cat#: 585104 | Name: Ritlecitinib tosylate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Ritlecitinib tosylate

CAS#2192215-81-7 (tosylate)

Theoretical Analysis

MedKoo Cat#: 585104

Name: Ritlecitinib tosylate

CAS#: 2192215-81-7 (tosylate)

Chemical Formula: C22H27N5O4S

Exact Mass: 0.0000

Molecular Weight: 457.55

Elemental Analysis: C, 57.75; H, 5.95; N, 15.31; O, 13.99; S, 7.01

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,150.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Related CAS #

1792180-81-4 (free base) 2140301-97-7 (malonate) 2192215-81-7 (tosylate) 2489392-29-0 (maleate)

Synonym

Ritlecitinib tosylate; Ritlecitinib; PF-06651600; PF 06651600; PF06651600; PF-6651600; PF 6651600; PF6651600;

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

InChi Key

YOZLVAFWYLSRRN-VZXYPILPSA-N

InChi Code

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

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

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.

Storage Condition

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

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 457.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Bauman JN, Doran AC, Gualtieri GM, Hee B, Strelevitz T, Cerny MA, Banfield C, Plotka A, Wang X, Purohit VS, Dowty ME. The Pharmacokinetics, Metabolism, and Clearance Mechanisms of Ritlecitinib, a Janus Kinase 3 and Tyrosine-Protein Kinase Family Inhibitor, in Humans. Drug Metab Dispos. 2024 Aug 7:DMD- AR-2024-001843. doi: 10.1124/dmd.124.001843. Epub ahead of print. PMID: 39111823. 2: Gowda SK, Aggarwal A, Thakur V, Behera B, Garg S, Sethy M, Ayyanar P. Tofacitinib in Pediatric Alopecia Areata Totalis and Alopecia Universalis: A Retrospective Analysis From India. J Cutan Med Surg. 2024 Jul 26:12034754241266128. doi: 10.1177/12034754241266128. Epub ahead of print. PMID: 39056399. 3: Guan R, Lin Y, Zhang C, Wang Z, Wu Z, Liu X, Chen X, Piao Y. Comparative efficacy and safety of systemic steroids, oral JAK inhibitors and Contact Immunotherapy in the Treatment of severe alopecia areata: a systematic review and network meta-analysis. Arch Dermatol Res. 2024 Jul 23;316(7):483. doi: 10.1007/s00403-024-03177-9. PMID: 39042154. 4: Yamaguchi Y, Peeva E, Duca ED, Facheris P, Bar J, Shore R, Cox LA, Sloan A, Thaçi D, Ganesan A, Han G, Ezzedine K, Ye Z, Guttman-Yassky E. Ritlecitinib, a JAK3/TEC family kinase inhibitor, stabilizes active lesions and repigments stable lesions in vitiligo. Arch Dermatol Res. 2024 Jul 18;316(7):478. doi: 10.1007/s00403-024-03182-y. PMID: 39023568; PMCID: PMC11258076. 5: Mansilla-Polo M, Morgado-Carrasco D. Biologics Versus JAK Inhibitors. Part II: Risk of Infections. A Narrative Review. Dermatol Ther (Heidelb). 2024 Aug;14(8):1983-2038. doi: 10.1007/s13555-024-01203-2. Epub 2024 Jul 16. PMID: 39014279; PMCID: PMC11333430. 6: Verstockt B. VIBRATO's Symphony: Orchestrating Biomarker Harmony for Ritlecitinib in UC Therapy. J Crohns Colitis. 2024 Jul 5:jjae103. doi: 10.1093/ecco-jcc/jjae103. Epub ahead of print. PMID: 38970386. 7: Anderson S, Cavaletti G, Hood LJ, Polydefkis M, Herrmann DN, Rance G, King B, McMichael AJ, Senna MM, Kim BS, Napatalung L, Wolk R, Zwillich SH, Schaefer G, Gong Y, Sisson M, Posner HB. A phase 2a study investigating the effects of ritlecitinib on brainstem auditory evoked potentials and intraepidermal nerve fiber histology in adults with alopecia areata. Pharmacol Res Perspect. 2024 Aug;12(4):e1204. doi: 10.1002/prp2.1204. PMID: 38969959; PMCID: PMC11226387. 8: Lloyd A, Aggio D, Dixon C, Law EH, Price T. Psychometric Properties of the EQ-5D-5L in Patients with Alopecia Areata. Pharmacoecon Open. 2024 Jul 6. doi: 10.1007/s41669-024-00504-8. Epub ahead of print. PMID: 38969921. 9: Sinclair R, Law EH, Zhang X, Zhang F, Napatalung L, Zwillich SH, King B, Mesinkovska N. Patient-Reported Satisfaction with Hair Regrowth in a Study of Ritlecitinib in Alopecia Areata: Results from ALLEGRO-2b/3. Dermatology. 2024 Jun 27:1-11. doi: 10.1159/000539536. Epub ahead of print. PMID: 38934147. 10: Song CJ, Riley CA, Wilkison BD, Cho S. A Review of JAK Inhibitors for Treatment of Alopecia Areata in the Military Health Care System. Mil Med. 2024 Jun 8:usae292. doi: 10.1093/milmed/usae292. Epub ahead of print. PMID: 38850223. 11: ▼Ritlecitinib for severe alopecia areata. Drug Ther Bull. 2024 May 29;62(6):87-92. doi: 10.1136/dtb.2024.000014. PMID: 38811041. 12: King B, Soung J, Tziotzios C, Rudnicka L, Joly P, Gooderham M, Sinclair R, Mesinkovska NA, Paul C, Gong Y, Anway SD, Tran H, Wolk R, Zwillich SH, Lejeune A. Correction to: Integrated Safety Analysis of Ritlecitinib, an Oral JAK3/TEC Family Kinase Inhibitor, for the Treatment of Alopecia Areata from the ALLEGRO Clinical Trial Program. Am J Clin Dermatol. 2024 Jul;25(4):689. doi: 10.1007/s40257-024-00864-1. Erratum for: Am J Clin Dermatol. 2024 Mar;25(2):299-314. doi: 10.1007/s40257-024-00846-3. PMID: 38789821; PMCID: PMC11193833. 13: Bushwereb R, Srivastava G. Exploring Janus kinase inhibitors for alopecia areata: a comprehensive review. Ital J Dermatol Venerol. 2024 Aug;159(4):380-389. doi: 10.23736/S2784-8671.24.07894-0. Epub 2024 May 23. PMID: 38780910. 14: Ding YW, Li Y, Zhang ZW, Dao JW, Wei DX. Hydrogel forming microneedles loaded with VEGF and Ritlecitinib/polyhydroxyalkanoates nanoparticles for mini- invasive androgenetic alopecia treatment. Bioact Mater. 2024 Apr 23;38:95-108. doi: 10.1016/j.bioactmat.2024.04.020. PMID: 38699241; PMCID: PMC11061199. 15: Chim I, Ghiya R, Sinclair RD, Eisman S. Novel investigational drugs for alopecia areata and future perspectives. Expert Opin Investig Drugs. 2024 May;33(5):441-449. doi: 10.1080/13543784.2024.2348062. Epub 2024 May 20. PMID: 38682280. 16: Yan T, Wang T, Tang M, Liu N. Comparative efficacy and safety of JAK inhibitors in the treatment of moderate-to-severe alopecia areata: a systematic review and network meta-analysis. Front Pharmacol. 2024 Apr 10;15:1372810. doi: 10.3389/fphar.2024.1372810. PMID: 38659584; PMCID: PMC11039836. 17: Pranić S, Pulumati A, Vuković D. Protocol for a systematic review and meta- analysis on Janus kinase inhibitors in the management of vitiligo. Syst Rev. 2024 Apr 19;13(1):110. doi: 10.1186/s13643-024-02522-3. PMID: 38641831; PMCID: PMC11027385. 18: Hossain MM, Khalid A, Akhter Z, Parveen S, Ayaz MO, Bhat AQ, Badesra N, Showket F, Dar MS, Ahmed F, Dhiman S, Kumar M, Singh U, Hussain R, Keshari P, Mustafa G, Nargorta A, Taneja N, Gupta S, Mir RA, Kshatri AS, Nandi U, Khan N, Ramajayan P, Yadav G, Ahmed Z, Singh PP, Dar MJ. Discovery of a novel and highly selective JAK3 inhibitor as a potent hair growth promoter. J Transl Med. 2024 Apr 18;22(1):370. doi: 10.1186/s12967-024-05144-4. PMID: 38637842; PMCID: PMC11025159. 19: Wojciechowski J, Mukherjee A, Banfield C, Nicholas T. Model-Informed Assessment of Probability of Phase 3 Success for Ritlecitinib in Patients with Moderate-to-Severe Ulcerative Colitis. Clin Pharmacol Ther. 2024 Sep;116(3):724-735. doi: 10.1002/cpt.3251. Epub 2024 Apr 16. PMID: 38627914. 20: Utama A, Wijesinghe R, Thng S. Janus kinase inhibitors and the changing landscape of vitiligo management: a scoping review. Int J Dermatol. 2024 Aug;63(8):1020-1035. doi: 10.1111/ijd.17157. Epub 2024 Apr 12. PMID: 38610078.

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Description:

Chemical Structure

Theoretical Analysis

Price and Availability

Preparing Stock Solutions

View History

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