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MedKoo Cat#: 555328 | Name: PF-06651600 free base
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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

PF-06651600 free base
PF-06651600 free base
CAS#1792180-81-4 (free base)

Theoretical Analysis

MedKoo Cat#: 555328

Name: PF-06651600 free base

CAS#: 1792180-81-4 (free base)

Chemical Formula: C15H19N5O

Exact Mass: 285.1590

Molecular Weight: 285.35

Elemental Analysis: C, 63.14; H, 6.71; N, 24.54; O, 5.61

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
50mg USD 250.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,250.00 Ready to ship
1g USD 1,950.00 Ready to ship
2g USD 3,250.00 2 Weeks
5g 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; 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-ylamino)-1-piperidinyl]-2-propen-1-one
InChi Key
CBRJPFGIXUFMTM-WDEREUQCSA-N
InChi Code
InChI=1S/C15H19N5O/c1-3-13(21)20-8-11(5-4-10(20)2)19-15-12-6-7-16-14(12)17-9-18-15/h3,6-7,9-11H,1,4-5,8H2,2H3,(H2,16,17,18,19)/t10-,11+/m0/s1
SMILES Code
C=CC(N1[C@@H](C)CC[C@@H](NC2=C3C(NC=C3)=NC=N2)C1)=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
Biological target:
Ritlecitinib (PF-06651600) is a JAK3 inhibitor with an IC50 of 33.1 nM.
In vitro activity:
In vitro, PF-06651600 inhibited Th1 and Th17 cell differentiation and function. Importantly, by sparing JAK1 function, PF-06651600 selectively targeted γc cytokine pathways while preserving JAK1-dependent anti-inflammatory signaling such as the IL-10 suppressive functions following LPS treatment in macrophages and the suppression of TNFα and IL-1β production in IL-27-primed macrophages. Reference: ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. https://pubs.acs.org/doi/10.1021/acschembio.6b00677
In vivo activity:
In vivo, PF-06651600 reduced disease pathology in rat adjuvant-induced arthritis as well as in mouse experimental autoimmune encephalomyelitis models. Reference: ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. https://pubs.acs.org/doi/10.1021/acschembio.6b00677
Solvent mg/mL mM
Solubility
DMSO 100.0 350.40
H2O 5.0 17.50
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 285.35 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. 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.
In vitro protocol:
1. 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.
In vivo protocol:
1. 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.
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.