1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

Peficitinib (Synonyms: ASP015K; JNJ-54781532; ASP-015K; ASP 015K; JNJ54781532; JNJ 54781532)

Cat. No.: HY-19568 Purity: 99.86%
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Peficitinb (ASP015K, JNJ-54781532) is a novel oral Janus kinase (JAK) inhibitor. Peficitinib inhibits JAK1, JAK2, JAK3 and Tyk2 enzyme activities with IC50s of 3.9, 5.0, 0.71 and 4.8 nM, respectively, and has moderate selectivity for JAK3 inhibition.

For research use only. We do not sell to patients.
Peficitinib Chemical Structure

Peficitinib Chemical Structure

CAS No. : 944118-01-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $180 In-stock
25 mg $320 In-stock
50 mg $590 In-stock
100 mg $990 In-stock
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Description

Peficitinb (ASP015K, JNJ-54781532) is a novel oral Janus kinase (JAK) inhibitor. Peficitinib inhibits JAK1, JAK2, JAK3 and Tyk2 enzyme activities with IC50s of 3.9, 5.0, 0.71 and 4.8 nM, respectively, and has moderate selectivity for JAK3 inhibition. IC50 value: 3.9/5.0/0.71 nM (for JAK1/2/3) , 4.8 nM (for Tyk2) Target: JAK Peficitinib (ASP015K) is a novel orally bioavailable JAK inhibitor in development for the treatment of severe rheumatoid arthritis (RA). Milder inhibition of JAK2 by Peficitinib may contribute to the mitigation of effects on red blood cells and platelets reported to be caused by JAK2 inhibition. Moreover, Peficitinib has shown an improvement in symptoms in RA animal models after once-daily oral administration, and has demonstrated dose-dependent improvement in psoriatic disease activities in a 6-week phase IIa study. The terminal mean half-life of Peficitinib was estimated to be 7-13 h in pharmacological studies with healthy subjects, suggesting that Peficitinib can be dosed once-daily in the next development stage.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02111317 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K October 2013 Phase 1
NCT01929577 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Bioavailability of ASP015K|Healthy Subjects|Pharmacokinetics of ASP015K|Food Effect of ASP015K May 2013 Phase 1
NCT01486017 Astellas Pharma Inc Bioavailability of ASP015K|Pharmacokinetics of ASP015K|Healthy Subjects September 2011 Phase 1
NCT01406132 Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K December 2009 Phase 1
NCT02141425 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Healthy Volunteers|Pharmacokinetics of ASP015K March 2014 Phase 1
NCT01959399 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K May 2013 Phase 1
NCT01686217 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Pharmacokinetics of ASP015K|Food Effect|Healthy Volunteers June 2012 Phase 1
NCT02531191 Astellas Pharma Inc Healthy Volunteers June 2015 Phase 1
NCT01182077 Astellas Pharma Inc Healthy|Pharmacokinetics of ASP015K and Midazolam June 2010 Phase 1
NCT01638013 Astellas Pharma Inc Arthritis, Rheumatoid June 13, 2012 Phase 3
NCT01225224 Astellas Pharma Inc Healthy Volunteer|Pharmacokinetics of ASP015K November 2009 Phase 1
NCT01711814 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Arthritis, Rheumatoid September 2012 Phase 2
NCT02760342 Astellas Pharma Inc Healthy Subjects May 2016 Phase 1
NCT01484964 Astellas Pharma Inc Pharmacokinetics of ASP015K|Bioavailability of ASP015K|Healthy Subjects September 2011 Phase 1
NCT01190670 Astellas Pharma Inc Healthy|Pharmacokinetics of ASP015K and Tacrolimus July 2010 Phase 1
NCT01364987 Astellas Pharma Inc Healthy Subjects|Drug Interactions|Pharmacokinetics of ASP015K May 2009 Phase 1
NCT01554696 Astellas Pharma Inc Arthritis, Rheumatoid June 2012 Phase 2
NCT01430065 Astellas Pharma Inc Pharmacokinetics of ASP015K|Drug Interactions|Healthy Subjects June 2009 Phase 1
NCT01565655 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Arthritis, Rheumatoid June 2012 Phase 2
NCT01754805 Astellas Pharma Inc Rheumatoid Arthritis February 2010 Phase 1
NCT01364974 Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K|Pharmacodynamics January 2009 Phase 1
NCT01387087 Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K July 2008 Phase 1
NCT01430078 Astellas Pharma Inc Healthy September 2010 Phase 1
NCT02305849 Astellas Pharma Inc Rheumatoid Arthritis July 25, 2014 Phase 3
NCT01649999 Astellas Pharma Inc Arthritis, Rheumatoid February 2012 Phase 2
NCT01096862 Astellas Pharma Inc Psoriasis March 2010 Phase 2
NCT02308163 Astellas Pharma Inc Rheumatoid Arthritis July 2014 Phase 3
NCT02586194 Astellas Pharma Inc Patients With Impaired Hepatic Function November 2015 Phase 1
NCT02603497 Astellas Pharma Inc Patients With Impaired Renal Function November 2015 Phase 1
NCT02111317 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K October 2013 Phase 1
NCT01929577 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Bioavailability of ASP015K|Healthy Subjects|Pharmacokinetics of ASP015K|Food Effect of ASP015K May 2013 Phase 1
NCT01486017 Astellas Pharma Inc Bioavailability of ASP015K|Pharmacokinetics of ASP015K|Healthy Subjects September 2011 Phase 1
NCT01406132 Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K December 2009 Phase 1
NCT02141425 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Healthy Volunteers|Pharmacokinetics of ASP015K March 2014 Phase 1
NCT01959399 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K May 2013 Phase 1
NCT01686217 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Pharmacokinetics of ASP015K|Food Effect|Healthy Volunteers June 2012 Phase 1
NCT02531191 Astellas Pharma Inc Healthy Volunteers June 2015 Phase 1
NCT01182077 Astellas Pharma Inc Healthy|Pharmacokinetics of ASP015K and Midazolam June 2010 Phase 1
NCT01638013 Astellas Pharma Inc Arthritis, Rheumatoid June 13, 2012 Phase 3
NCT01225224 Astellas Pharma Inc Healthy Volunteer|Pharmacokinetics of ASP015K November 2009 Phase 1
NCT01711814 Astellas Pharma Global Development, Inc.|Janssen Biotech, Inc.|Astellas Pharma Inc Arthritis, Rheumatoid September 2012 Phase 2
NCT02760342 Astellas Pharma Inc Healthy Subjects May 2016 Phase 1
NCT01484964 Astellas Pharma Inc Pharmacokinetics of ASP015K|Bioavailability of ASP015K|Healthy Subjects September 2011 Phase 1
NCT01190670 Astellas Pharma Inc Healthy|Pharmacokinetics of ASP015K and Tacrolimus July 2010 Phase 1
NCT01364987 Astellas Pharma Inc Healthy Subjects|Drug Interactions|Pharmacokinetics of ASP015K May 2009 Phase 1
NCT01554696 Astellas Pharma Inc Arthritis, Rheumatoid June 2012 Phase 2
NCT01430065 Astellas Pharma Inc Pharmacokinetics of ASP015K|Drug Interactions|Healthy Subjects June 2009 Phase 1
NCT01565655 Astellas Pharma Global Development, Inc.|Astellas Pharma Inc Arthritis, Rheumatoid June 2012 Phase 2
NCT01754805 Astellas Pharma Inc Rheumatoid Arthritis February 2010 Phase 1
NCT01364974 Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K|Pharmacodynamics January 2009 Phase 1
NCT01387087 Astellas Pharma Inc Healthy Subjects|Pharmacokinetics of ASP015K July 2008 Phase 1
NCT01430078 Astellas Pharma Inc Healthy September 2010 Phase 1
NCT02305849 Astellas Pharma Inc Rheumatoid Arthritis July 25, 2014 Phase 3
NCT01649999 Astellas Pharma Inc Arthritis, Rheumatoid February 2012 Phase 2
NCT01096862 Astellas Pharma Inc Psoriasis March 2010 Phase 2
NCT02308163 Astellas Pharma Inc Rheumatoid Arthritis July 2014 Phase 3
NCT02586194 Astellas Pharma Inc Patients With Impaired Hepatic Function November 2015 Phase 1
NCT02603497 Astellas Pharma Inc Patients With Impaired Renal Function November 2015 Phase 1
NCT01959282 Janssen Research & Development, LLC Colitis, Ulcerative November 2013 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 3.0638 mL 15.3191 mL 30.6382 mL
5 mM 0.6128 mL 3.0638 mL 6.1276 mL
10 mM 0.3064 mL 1.5319 mL 3.0638 mL
References
M.Wt

326.39

Formula

C₁₈H₂₂N₄O₂

CAS No.

944118-01-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 60 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Peficitinib
Cat. No.:
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