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Peficitinib（ASP015K,JNJ-54781532）

  Cat. No.:  DC8168   Featured
Chemical Structure
944118-01-8
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More than 5000 active chemicals with high quality for research!
Field of application
Peficitinib(ASP015K,JNJ-54781532) is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 944118-01-8
Chemical Name: Peficitinib
Synonyms: peficitinib;4-[[(1R,3S)-5-hydroxy-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide;ASP015K;ASP-015K;4-[(trans-5-Hydroxyadamantan-2-yl)amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide;ASP 015K;Peficitinib free base;HPH1166CKX;4-(((1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl)amino)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide;4-[[(1S,3R)-5-oxidanyl-2-adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide;Peficitinib [USAN:INN];9T6;Peficitinib (USAN/INN);GTPL8315;stereoisomer of 4-[(5-Hydroxytricyclo[3.3.1.13,7]dec-2-yl)amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide (ACI);4-[(anti-5-Hydroxyadamantan-2-yl)amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide;JNJ 54781532
SMILES: N(C1=C(C(=O)N)C=NC2NC=CC1=2)[C@@H]1[C@@H]2CC3CC(C2)(O)C[C@H]1C3
Formula: C18H22N4O2
M.Wt: 326.392883777618
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
In Vivo: Peficitinib (20 mg/kg, p.o.) suppresses IL-2-induced STAT5 phosphorylation by 78% in the rat model of adjuvant-induced arthritis (AIA). Peficitinib potently inhibits the increase in paw volume (≥1 mg/kg) with an ED50 of 2.7 mg/kg, significantly reduces the bone destruction score (≥10 mg/kg) and almost fully ameliorates both paw swelling and bone destruction scores (30 mg/kg)[1].
In Vitro: Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Peficitinib inhibits IL-2-induced T cell proliferation with an IC50 of 10 nM. Peficitinib also suppresses the IL-2-induced STAT5 phosphorylation in rat and human whole blood, with mean IC50s of 124 nM and 127 nM, respectively[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC10431 Upadacitinib Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.
DC5165 Tofacitinib (CP-690550) Citrate Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC8736 Tofacitinib Tofacitinib is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent versus JAK2 and JAK1. Phase 3.
DC10779 PF-06651600 PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.
DC8168 Peficitinib（ASP015K,JNJ-54781532） Peficitinib(ASP015K,JNJ-54781532) is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats.
DC7137 Filgotinib(GLPG0634) Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
DC8171 Decernotinib (VX-509,adelatinib) Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
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