Peficitinib | ASP015K | JNJ-54781532 | CAS#944118-01-8 | JAK inhibitor

MedKoo Cat#: 206125 | Name: Peficitinib free base

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 free base

CAS#944118-01-8 (free base)

Theoretical Analysis

MedKoo Cat#: 206125

Name: Peficitinib free base

CAS#: 944118-01-8 (free base)

Chemical Formula: C18H22N4O2

Exact Mass: 326.1743

Molecular Weight: 326.39

Elemental Analysis: C, 66.24; H, 6.79; N, 17.17; O, 9.80

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,350.00	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; ASP015K; ASP015K; ASP 015K; JNJ54781532; JNJ54781532; JNJ 54781532.

IUPAC/Chemical Name

4-(((1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl)amino)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide

InChi Key

DREIJXJRTLTGJC-KDJQDEFKSA-N

InChi Code

InChI=1S/C18H22N4O2/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)/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

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, not in water

Shelf Life

>2 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 326.39 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

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PMID: 38905267; PMCID: PMC11192398. 4: Potlabathini T, Pothacamuri MA, Bandi VV, Anjum M, Shah P, Molina M, Dutta N, Adzhymuratov O, Mathew M, Sadu V, Zahid SA, Lingamgunta H, Sahotra M, Nasiri SMZJ, Daguipa CDM. FDA-Approved Janus Kinase-Signal Transducer and Activator of Transcription (JAK-STAT) Inhibitors for Managing Rheumatoid Arthritis: A Narrative Review of the Literature. Cureus. 2024 May 9;16(5):e59978. doi: 10.7759/cureus.59978. PMID: 38854342; PMCID: PMC11162266. 5: Cai W, Tong R, Sun Y, Yao Y, Zhang J. Comparative efficacy of five approved Janus kinase inhibitors as monotherapy and combination therapy in patients with moderate-to-severe active rheumatoid arthritis: a systematic review and network meta-analysis of randomized controlled trials. Front Pharmacol. 2024 Apr 24;15:1387585. doi: 10.3389/fphar.2024.1387585. PMID: 38725657; PMCID: PMC11080655. 6: Amaral JL, Lucredi NC, França VLB, Santos SJM, Maia FF Jr, Morais PA, Souza PFN, Comar JF, Freire VN. Tofacitinib and peficitinib inhibitors of Janus kinase for autoimmune disease treatment: a quantum biochemistry approach. Phys Chem Chem Phys. 2024 May 1;26(17):13420-13431. doi: 10.1039/d3cp06332a. PMID: 38647171. 7: Jiang W, Ren J, Li X, Yang J, Cheng D. Peficitinib alleviated acute lung injury by blocking glycolysis through JAK3/STAT3 pathway. Int Immunopharmacol. 2024 May 10;132:111931. doi: 10.1016/j.intimp.2024.111931. Epub 2024 Mar 27. PMID: 38547769. 8: Yang Y, Li J, Liu J, Liu L, Wang Y, Hu J, Li Z, Gu J, Zhang X, Xiao Z, Zheng J, Liu L, Li Z, Wei JC. Safety and efficacy of peficitinib in Asian patients with rheumatoid arthritis who had an inadequate response or intolerance to methotrexate: results of a multicenter, randomized, double-blind, placebo- controlled phase 3 study. Lancet Reg Health West Pac. 2023 Oct 18;42:100925. doi: 10.1016/j.lanwpc.2023.100925. PMID: 38357391; PMCID: PMC10865021. 9: Tanaka Y, Takeuchi T, Morita Y, Kaneko Y, Terada W. Safety and effectiveness of peficitinib 100 mg/day in patients achieving clinical remission from a long- term open-label extension study in Japan, Korea, and Taiwan (RAJ2). Mod Rheumatol. 2023 Dec 7:road110. doi: 10.1093/mr/road110. Epub ahead of print. PMID: 38103258. 10: Hayashi S, Tachibana S, Maeda T, Yamashita M, Shirasugi I, Yamamoto Y, Yamada H, Okano T, Nishimura K, Ueda Y, Jinnno S, Saegusa J, Yamamoto W, Murata K, Fujii T, Hata K, Yoshikawa A, Ebina K, Etani Y, Yoshida N, Amuro H, Hashimoto M, Hara R, Katayama M, Okano T, Kuroda R. Real-world comparative study of the efficacy of Janus kinase inhibitors in patients with rheumatoid arthritis: the ANSWER cohort study. Rheumatology (Oxford). 2023 Nov 1:kead543. doi: 10.1093/rheumatology/kead543. Epub ahead of print. Erratum in: Rheumatology (Oxford). 2024 Feb 13:keae095. doi: 10.1093/rheumatology/keae095. PMID: 37924201. 11: Takeuchi T, Tanaka Y, Morita Y, Kato D, Kaneko Y, Terada W. Association between matrix metalloprotease-3 levels and radiographic progression in patients with RA: a post hoc analysis from a Japanese phase 3 clinical trial of peficitinib (RAJ4). Mod Rheumatol. 2023 Oct 30:road102. doi: 10.1093/mr/road102. Epub ahead of print. PMID: 37902304. 12: Taylor PC, Choy E, Baraliakos X, Szekanecz Z, Xavier RM, Isaacs JD, Strengholt S, Parmentier JM, Lippe R, Tanaka Y. Differential properties of Janus kinase inhibitors in the treatment of immune-mediated inflammatory diseases. Rheumatology (Oxford). 2024 Feb 1;63(2):298-308. doi: 10.1093/rheumatology/kead448. PMID: 37624925; PMCID: PMC10836981. 13: Xu Q, He L, Yin Y. Risk of herpes zoster associated with JAK inhibitors in immune-mediated inflammatory diseases: a systematic review and network meta- analysis. Front Pharmacol. 2023 Aug 8;14:1241954. doi: 10.3389/fphar.2023.1241954. PMID: 37614317; PMCID: PMC10442487. 14: Xia D, Xu X, Wei J, Wang W, Xiong J, Tan Q, Xue P, Wang H. CHAF1A promotes the proliferation and growth of epithelial ovarian cancer cells by affecting the phosphorylation of JAK2/STAT3 signaling pathway. Biochem Biophys Rep. 2023 Jul 31;35:101522. doi: 10.1016/j.bbrep.2023.101522. PMID: 37575547; PMCID: PMC10415620. 15: He S, Xia J, Jia H, Dai Q, Chen C, Zhou Y, Wang XB. Peficitinib ameliorates 5-fluorouracil-induced intestinal damage by inhibiting aging, inflammatory factors and oxidative stress. Int Immunopharmacol. 2023 Oct;123:110753. doi: 10.1016/j.intimp.2023.110753. Epub 2023 Aug 10. PMID: 37572505. 16: Roskoski R Jr. Small molecule protein kinase inhibitors approved by regulatory agencies outside of the United States. Pharmacol Res. 2023 Aug;194:106847. doi: 10.1016/j.phrs.2023.106847. Epub 2023 Jul 15. PMID: 37454916. 17: Hua H, Zhao Q, Xia J, Dai QL, Bai SR, Wang XB, Zhou M. Peficitinib ameliorates doxorubicin-induced cardiotoxicity by suppressing cellular senescence and enhances its antitumor activity. Int Immunopharmacol. 2023 Sep;122:110630. doi: 10.1016/j.intimp.2023.110630. Epub 2023 Jul 12. PMID: 37451017. 18: Tanaka Y, Takeuchi T, Morita Y, Kato D, Kaneko Y, Terada W. Post hoc analysis of patients with rheumatoid arthritis under clinical remission in two Japanese Phase 3 trials of peficitinib treatment (RAJ3 and RAJ4). Mod Rheumatol. 2024 Mar 28;34(3):453-465. doi: 10.1093/mr/road059. PMID: 37319017. 19: Russell MD, Stovin C, Alveyn E, Adeyemi O, Chan CKD, Patel V, Adas MA, Atzeni F, Ng KKH, Rutherford AI, Norton S, Cope AP, Galloway JB. JAK inhibitors and the risk of malignancy: a meta-analysis across disease indications. Ann Rheum Dis. 2023 Aug;82(8):1059-1067. doi: 10.1136/ard-2023-224049. Epub 2023 May 29. PMID: 37247942; PMCID: PMC10359573. 20: Oba Y, Sawa N, Ikuma D, Mizuno H, Inoue N, Sekine A, Hasegawa E, Yamanouchi M, Suwabe T, Yamaguchi Y, Takasawa Y, Ubara Y. Successful peficitinib monotherapy for the new-onset skin manifestations of rheumatoid vasculitis after long-term treatment with tocilizumab for rheumatoid arthritis. Mod Rheumatol Case Rep. 2023 Dec 29;8(1):5-10. doi: 10.1093/mrcr/rxad025. PMID: 37210210.