Ropsacitinib
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MedKoo CAT#: 555579

CAS#: 2127109-84-4

Description: 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

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Ropsacitinib
CAS# 2127109-84-4
Instruction

Theoretical Analysis

MedKoo Cat#: 555579
Name: Ropsacitinib
CAS#: 2127109-84-4
Chemical Formula: C20H17N9
Exact Mass: 383.16
Molecular Weight: 383.419
Elemental Analysis: C, 62.65; H, 4.47; N, 32.88

Price and Availability

Size Price Availability Quantity
5mg USD 750 2 Weeks
10mg USD 1250 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:

Biological target:
In vitro activity:
In vivo activity:

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.

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:
In vitro protocol:
In vivo protocol:

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1: 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.


2: 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.


3: Tehlirian C, Singh RSP, Pradhan V, Roberts ES, Tarabar S, Peeva E, Vincent MS, Gale JD. Oral tyrosine kinase 2 inhibitor PF-06826647 demonstrates efficacy and an acceptable safety profile in participants with moderate-to-severe plaque psoriasis in a phase 2b, randomized, double-blind, placebo-controlled study. J Am Acad Dermatol. 2022 Aug;87(2):333-342. doi: 10.1016/j.jaad.2022.03.059. Epub 2022 Apr 6. PMID: 35398218.


4: Krueger JG, McInnes IB, Blauvelt A. Tyrosine kinase 2 and Janus kinase‒signal transducer and activator of transcription signaling and inhibition in plaque psoriasis. J Am Acad Dermatol. 2022 Jan;86(1):148-157. doi: 10.1016/j.jaad.2021.06.869. Epub 2021 Jul 2. PMID: 34224773.


5: Danese S, Peyrin-Biroulet L. Selective Tyrosine Kinase 2 Inhibition for Treatment of Inflammatory Bowel Disease: New Hope on the Rise. Inflamm Bowel Dis. 2021 Nov 15;27(12):2023-2030. doi: 10.1093/ibd/izab135. PMID: 34089259; PMCID: PMC8599029.


6: Jo CE, Gooderham M, Beecker J. TYK 2 inhibitors for the treatment of dermatologic conditions: the evolution of JAK inhibitors. Int J Dermatol. 2022 Feb;61(2):139-147. doi: 10.1111/ijd.15605. Epub 2021 Apr 30. PMID: 33929045.


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.


8: Gerstenberger BS, Ambler C, Arnold EP, Banker ME, Brown MF, Clark JD, Dermenci A, Dowty ME, Fensome A, Fish S, Hayward MM, Hegen M, Hollingshead BD, Knafels JD, Lin DW, Lin TH, Owen DR, Saiah E, Sharma R, Vajdos FF, Xing L, Yang X, Yang X, Wright SW. Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases. J Med Chem. 2020 Nov 25;63(22):13561-13577. doi: 10.1021/acs.jmedchem.0c00948. Epub 2020 Aug 25. PMID: 32787094.


9: Nogueira M, Puig L, Torres T. JAK Inhibitors for Treatment of Psoriasis: Focus on Selective TYK2 Inhibitors. Drugs. 2020 Mar;80(4):341-352. doi: 10.1007/s40265-020-01261-8. PMID: 32020553.