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.
Cas No.: 944118-01-8
Chemical Name: 4-{[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]amino}-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
Synonyms: ASP015K,JNJ-54781532
SMILES: 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
Formula: C18H22N4O2
M.Wt: 326.17
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) GPLG0634 is a novel inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
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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