Ropsacitinib | CAS# 2127109-84-4 | TYK2 inhibitor

MedKoo Cat#: 555579 | Name: Ropsacitinib

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Description:

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

ropsacitinib, also known as PF-06826647 and Tyk2-IN-8, is an orally administered, tyrosine kinase 2 (TYK2) inhibitor, that is in development with Pfizer for the treatment of plaque psoriasis and inflammatory bowel disease.

Chemical Structure

Ropsacitinib

CAS#2127109-84-4

Theoretical Analysis

MedKoo Cat#: 555579

Name: Ropsacitinib

CAS#: 2127109-84-4

Chemical Formula: C20H17N9

Exact Mass: 383.1607

Molecular Weight: 383.42

Elemental Analysis: C, 62.65; H, 4.47; N, 32.88

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 750.00	2 Weeks
10mg	USD 1,250.00	2 Weeks

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Related CAS #

2127109-85-5 (cis-isomer) 2127109-84-4

Synonym

PF-06826647; PF 06826647; PF06826647; PF-6826647; PF 6826647; PF6826647; Tyk2-IN-8; Tyk2-IN 8; Tyk2-IN8; Ropsacitinib;

IUPAC/Chemical Name

(1r,3r)-3-(cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile

InChi Key

XPLZTJWZDBFWDE-OYOVHJISSA-N

InChi Code

InChI=1S/C20H17N9/c1-27-11-15(9-24-27)17-13-28-18(2-5-23-28)19(26-17)16-10-25-29(12-16)20(3-4-21)6-14(7-20)8-22/h2,5,9-14H,3,6-7H2,1H3/t14-,20-

SMILES Code

N#C[C@@H]1C[C@@](CC#N)(N2N=CC(C3=NC(C4=CN(C)N=C4)=CN5N=CC=C35)=C2)C1

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 383.42 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: Morand E, Merola JF, Tanaka Y, Gladman D, Fleischmann R. TYK2: an emerging therapeutic target in rheumatic disease. Nat Rev Rheumatol. 2024 Apr;20(4):232-240. doi: 10.1038/s41584-024-01093-w. Epub 2024 Mar 11. PMID: 38467779. 2: Kimball AB, Peeva E, Forman S, Moiin A, Khattri S, Porter ML, Mangold AR, Ghosh P, Banfield C, Oemar B. Brepocitinib, Zimlovisertib, and Ropsacitinib in Hidradenitis Suppurativa. NEJM Evid. 2024 Mar;3(3):EVIDoa2300155. doi: 10.1056/EVIDoa2300155. Epub 2024 Feb 9. PMID: 38335032. 3: Xu Y, Li Z, Wu S, Guo L, Jiang X. Oral small-molecule tyrosine kinase 2 and phosphodiesterase 4 inhibitors in plaque psoriasis: a network meta-analysis. Front Immunol. 2023 Jun 2;14:1180170. doi: 10.3389/fimmu.2023.1180170. PMID: 37334353; PMCID: PMC10272578. 4: Zhang K, Ye K, Tang H, Qi Z, Wang T, Mao J, Zhang X, Jiang S. Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors. J Med Chem. 2023 Apr 13;66(7):4378-4416. doi: 10.1021/acs.jmedchem.2c01800. Epub 2023 Mar 23. PMID: 36951608. 5: Martin G. Novel Therapies in Plaque Psoriasis: A Review of Tyrosine Kinase 2 Inhibitors. Dermatol Ther (Heidelb). 2023 Feb;13(2):417-435. doi: 10.1007/s13555-022-00878-9. Epub 2023 Jan 2. PMID: 36592300; PMCID: PMC9884727. 6: Loo WJ, Turchin I, Prajapati VH, Gooderham MJ, Grewal P, Hong CH, Sauder M, Vender RB, Maari C, Papp KA. Clinical Implications of Targeting the JAK-STAT Pathway in Psoriatic Disease: Emphasis on the TYK2 Pathway. J Cutan Med Surg. 2023 Jan-Feb;27(1_suppl):3S-24S. doi: 10.1177/12034754221141680. Epub 2022 Dec 15. PMID: 36519621. 7: Singh RSP, Pradhan V, Roberts ES, Scaramozza M, Kieras E, Gale JD, Peeva E, Vincent MS, Banerjee A, Fensome A, Dowty ME, Winkle P, Tehlirian C. Safety and Pharmacokinetics of the Oral TYK2 Inhibitor PF-06826647: A Phase I, Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation Study. Clin Transl Sci. 2021 Mar;14(2):671-682. doi: 10.1111/cts.12929. Epub 2020 Dec 8. PMID: 33290616; PMCID: PMC7993274.