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MedKoo Cat#: 592991 | Name: Peficitinib hydrobromide
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Description:

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

Peficitinib, also known as ASP015K and JNJ-54781532, is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats. ASP015K inhibited JAK1, JAK2, JAK3 and TYK2 enzyme activities with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM, respectively. ASP015K inhibited the IL-2-induced proliferation of human T cells with an IC50value of 18 nM. Moreover, ASP015K was 14-fold more potent against JAK1/3 than JAK2/2 on the basis of EPO-induced proliferation of human leukemia cells.

Chemical Structure

Peficitinib hydrobromide
Peficitinib hydrobromide
CAS#1353219-05-2 (HBr)

Theoretical Analysis

MedKoo Cat#: 592991

Name: Peficitinib hydrobromide

CAS#: 1353219-05-2 (HBr)

Chemical Formula: C18H23BrN4O2

Exact Mass: 0.0000

Molecular Weight: 407.31

Elemental Analysis: C, 53.08; H, 5.69; Br, 19.62; N, 13.76; O, 7.86

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 6,850.00 2 Weeks
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Related CAS #
1353219-05-2 (HBr) 944118-01-8 (free base)
Synonym
Peficitinib hydrobromide
IUPAC/Chemical Name
1H-Pyrrolo(2,3-b)pyridine-5-carboxamide, 4-((5-hydroxytricyclo(3.3.1.13,7)dec-2-yl)amino)-, hydrobromide (1:1), stereoisomer
InChi Key
ZUVPMAPXNYGJQC-ZVCJDZAXSA-N
InChi Code
InChI=1S/C18H22N4O2.BrH/c19-16(23)13-8-21-17-12(1-2-20-17)15(13)22-14-10-3-9-4-11(14)7-18(24,5-9)6-10;/h1-2,8-11,14,24H,3-7H2,(H2,19,23)(H2,20,21,22);1H/t9-,10-,11+,14-,18-;
SMILES Code
O=C(C1=CN=C(NC=C2)C2=C1N[C@@H]3[C@]4([H])C[C@@]5([H])C[C@](C4)(O)C[C@]3([H])C5)N.[H]Br
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

Preparing Stock Solutions

The following data is based on the product molecular weight 407.31 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
1: 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. Review. PubMed PMID: 29938545. 2: Sands BE, Sandborn WJ, Feagan BG, Lichtenstein GR, Zhang H, Strauss R, Szapary P, Johanns J, Panes J, Vermeire S, O'Brien CD, Yang Z, Bertelsen K, Marano C; Peficitinib-UC Study Group. Peficitinib, an Oral Janus Kinase Inhibitor, in Moderate-to-Severe Ulcerative Colitis: Results From a Randomized, Phase 2 Study. J Crohns Colitis. 2018 Jun 15. doi: 10.1093/ecco-jcc/jjy085. [Epub ahead of print] PubMed PMID: 29917064. 3: Veale DJ, McGonagle D, McInnes IB, Krueger JG, Ritchlin CT, Elewaut D, Kanik KS, Hendrikx T, Berstein G, Hodge J, Telliez JB. The rationale for Janus kinase inhibitors for the treatment of spondyloarthritis. Rheumatology (Oxford). 2018 Apr 3. doi: 10.1093/rheumatology/key070. [Epub ahead of print] PubMed PMID: 29618084. 4: Cline A, Cardwell LA, Feldman SR. Advances in treating psoriasis in the elderly with small molecule inhibitors. Expert Opin Pharmacother. 2017 Dec;18(18):1965-1973. doi: 10.1080/14656566.2017.1409205. Epub 2017 Nov 27. Review. PubMed PMID: 29171774. 5: Baker KF, Isaacs JD. Novel therapies for immune-mediated inflammatory diseases: What can we learn from their use in rheumatoid arthritis, spondyloarthritis, systemic lupus erythematosus, psoriasis, Crohn's disease and ulcerative colitis? Ann Rheum Dis. 2018 Feb;77(2):175-187. doi: 10.1136/annrheumdis-2017-211555. Epub 2017 Aug 1. Review. PubMed PMID: 28765121. 6: Zhu T, Howieson C, Wojtkowski T, Garg JP, Han D, Fisniku O, Keirns J. The Effect of Verapamil, a P-Glycoprotein Inhibitor, on the Pharmacokinetics of Peficitinib, an Orally Administered, Once-Daily JAK Inhibitor. Clin Pharmacol Drug Dev. 2017 Nov;6(6):548-555. doi: 10.1002/cpdd.344. Epub 2017 Mar 16. PubMed PMID: 28301084. 7: Genovese MC, Greenwald M, Codding C, Zubrzycka-Sienkiewicz A, Kivitz AJ, Wang A, Shay K, Wang X, Garg JP, Cardiel MH. Peficitinib, a JAK Inhibitor, in Combination With Limited Conventional Synthetic Disease-Modifying Antirheumatic Drugs in the Treatment of Moderate-to-Severe Rheumatoid Arthritis. Arthritis Rheumatol. 2017 May;69(5):932-942. doi: 10.1002/art.40054. PubMed PMID: 28118538. 8: Ito M, Yamazaki S, Yamagami K, Kuno M, Morita Y, Okuma K, Nakamura K, Chida N, Inami M, Inoue T, Shirakami S, Higashi Y. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33. doi: 10.1016/j.jphs.2016.12.001. Epub 2016 Dec 23. PubMed PMID: 28117214. 9: Zhu T, Parker B, Wojtkowski T, Nishimura T, Garg JP, Han D, Fisniku O, Keirns J. Drug Interactions Between Peficitinib, an Orally Administered, Once-Daily Janus Kinase Inhibitor, and Rosuvastatin in Healthy Subjects. Clin Pharmacokinet. 2017 Jul;56(7):747-757. doi: 10.1007/s40262-016-0474-4. PubMed PMID: 27878567. 10: Semerano L, Decker P, Clavel G, Boissier MC. Developments with investigational Janus kinase inhibitors for rheumatoid arthritis. Expert Opin Investig Drugs. 2016 Dec;25(12):1355-1359. Epub 2016 Oct 31. PubMed PMID: 27748152. 11: Kivitz AJ, Gutierrez-Ureña SR, Poiley J, Genovese MC, Kristy R, Shay K, Wang X, Garg JP, Zubrzycka-Sienkiewicz A. Peficitinib, a JAK Inhibitor, in the Treatment of Moderate-to-Severe Rheumatoid Arthritis in Patients With an Inadequate Response to Methotrexate. Arthritis Rheumatol. 2017 Apr;69(4):709-719. doi: 10.1002/art.39955. PubMed PMID: 27748083. 12: Lam S. JAK inhibitors: A broadening approach in rheumatoid arthritis. Drugs Today (Barc). 2016 Aug;52(8):467-469. PubMed PMID: 27722215. 13: Roskoski R Jr. Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol Res. 2016 Sep;111:784-803. doi: 10.1016/j.phrs.2016.07.038. Epub 2016 Jul 26. Review. PubMed PMID: 27473820. 14: Iwata S, Tanaka Y. Progress in understanding the safety and efficacy of Janus kinase inhibitors for treatment of rheumatoid arthritis. Expert Rev Clin Immunol. 2016 Oct;12(10):1047-57. doi: 10.1080/1744666X.2016.1189826. Epub 2016 Jun 6. Review. PubMed PMID: 27253519. 15: Cao YJ, Sawamoto T, Valluri U, Cho K, Lewand M, Swan S, Lasseter K, Matson M, Holman J Jr, Keirns J, Zhu T. Pharmacokinetics, Pharmacodynamics, and Safety of ASP015K (Peficitinib), a New Janus Kinase Inhibitor, in Healthy Subjects. Clin Pharmacol Drug Dev. 2016 Nov;5(6):435-449. doi: 10.1002/cpdd.273. Epub 2016 Jun 30. PubMed PMID: 27162173. 16: Nielsen OH, Seidelin JB, Ainsworth M, Coskun M. Will novel oral formulations change the management of inflammatory bowel disease? Expert Opin Investig Drugs. 2016 Jun;25(6):709-18. doi: 10.1517/13543784.2016.1165204. Epub 2016 Mar 28. Review. PubMed PMID: 26967267. 17: Yiu ZZ, Warren RB. Novel Oral Therapies for Psoriasis and Psoriatic Arthritis. Am J Clin Dermatol. 2016 Jun;17(3):191-200. doi: 10.1007/s40257-016-0179-3. Review. PubMed PMID: 26923915. 18: Takeuchi T, Tanaka Y, Iwasaki M, Ishikura H, Saeki S, Kaneko Y. Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K) monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled phase IIb study. Ann Rheum Dis. 2016 Jun;75(6):1057-64. doi: 10.1136/annrheumdis-2015-208279. Epub 2015 Dec 15. PubMed PMID: 26672064; PubMed Central PMCID: PMC4893099. 19: Oda K, Cao YJ, Sawamoto T, Nakada N, Fisniku O, Nagasaka Y, Sohda KY. Human mass balance, metabolite profile and identification of metabolic enzymes of [¹⁴C]ASP015K, a novel oral janus kinase inhibitor. Xenobiotica. 2015;45(10):887-902. doi: 10.3109/00498254.2015.1026864. Epub 2015 May 19. PubMed PMID: 25986538. 20: Nakada N, Oda K. Identification and characterization of metabolites of ASP015K, a novel oral Janus kinase inhibitor, in rats, chimeric mice with humanized liver, and humans. Xenobiotica. 2015;45(9):757-65. doi: 10.3109/00498254.2015.1019594. Epub 2015 Jun 12. PubMed PMID: 25869242.