A JAK inhibitor
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Peficitinib

Item No. 22954

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, stereoisomer
CAS Number
944118-01-8
Synonyms
  • ASP015K
  • JNJ-54781532
Molecular Formula
C18H22N4O2
Formula Weight
326.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 1 mg/ml
λmax
246, 294 nm
SMILES
NC(C1=CN=C2C(C=CN2)=C1N[C@@H]3[C@H](C4)C[C@@]5(O)C[C@@H]3C[C@@H]4C5)=O
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-
InChi Key
DREIJXJRTLTGJC-ZKVNVPQCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Peficitinib is an inhibitor of JAK (IC50s = 3.9, 5, and 0.71 nM for JAK1-3, respectively).1 It is 14-fold selective for JAK1 and JAK3 over JAK2 in erythropoietin-induced leukemia cell proliferation assays. Peficitinib inhibits IL-2-induced proliferation of rat splenocytes (IC50 = 10 nM) and phosphorylation of STAT5 in rat and human whole blood (IC50s = 124 and 127 nM, respectively).2 In vivo, peficitinib reduces paw swelling (ED50 = 5.6 mg/kg) and bone destruction in a rat model of adjuvant-induced arthritis when administered at a dose of 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Norman, P. Selective JAK inhibitors in development for rheumatoid arthritis. Expert Opin. Investig. Drugs 23(8), 1067-1077 (2014).

    2. Ito, M., Yamazaki, S., Yamagami, K., et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J. Pharmacol. Sci. 133(1), 25-33 (2017).