Peficitinib
- CAS No.
- 944118-01-8
- Chemical Name:
- Peficitinib
- Synonyms
- Carotegrast methyl;1H-Pyrrolo[2,3-b]pyridine-5-carboxamide, 4-[(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)amino]-, stereoisomer;CS-2584;Peficitinib;JNJ-54781532;JNJ-54781533;Peficitinib ASP015K;ASP015K;JNJ-54781532;Piraxostat Impurity 34;Peficitinb (ASP015K, JNJ-54781532)
- CBNumber:
- CB32730346
- Molecular Formula:
- C18H22N4O2
- Molecular Weight:
- 326.39
- MDL Number:
- MFCD28502035
- MOL File:
- 944118-01-8.mol
| storage temp. | Store at -20°C |
|---|---|
| solubility | Soluble in DMSO |
| form | Powder |
| FDA UNII | HPH1166CKX |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P280-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Peficitinib price More Price(23)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22954 | Peficitinib ≥98% | 944118-01-8 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 22954 | Peficitinib ≥98% | 944118-01-8 | 5mg | $161 | 2024-03-01 | Buy |
| Cayman Chemical | 22954 | Peficitinib ≥98% | 944118-01-8 | 10mg | $235 | 2024-03-01 | Buy |
| TRC | P218260 | Peficitinib | 944118-01-8 | 2.5mg | $110 | 2021-12-16 | Buy |
| ChemScene | CS-5393 | Peficitinib 99.78% | 944118-01-8 | 10mg | $150 | 2021-12-16 | Buy |
Peficitinib Chemical Properties,Uses,Production
Uses
Peficitinib can be used in therapeutic use and biological study of codrug and preparation of bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators.
Biological Activity
peficitinib (asp015k) is an oral janus kinase (jak) inhibitor. it inhibits enzyme activities of jak1, jak2, jak3 and tyk2 with ic50 values of 3.9, 5.0, 0.71 and 4.8 nmol/l, respectively. it showed moderate selectivity for jak3 inhibition [1].jak family of non-receptor protein tyrosine kinases includes jak1, jak2, jak3 and tyrosine kinase 2 (tyk2). jak1, jak2, jak3 and tyk2 are critically important in haematopoietic cells and immune cells [1].erythropoietin regulates haematopoiesis (the production of blood cells) [2]. treatment with asp015k inhibited the human t-cell proliferation induced by il-2. and this effect was greater than the effect to inhibit epo-induced human erythroleukemia cell proliferation. in human whole blood, asp015k concentration-dependently inhibited stat5 phosphorylation (pstat5) [3].in healthy volunteers, stat5-p was dose-dependently inhibited by asp015k. when the doses of asp015k were 60, 120, 200, or 300 mg, the mean peak percentage inhibitions of stat5-p were 84%, 85%, 92%, and 93%, respectively. plasma asp015k inhibited stat5-p with an ec50 value of 48 ng/ml, a shape factor (γ) of ~1.2, and an estimated emax close to 100%. on days 1, 7, and 14, at ~2 hours after treatment with asp015k at multiple doses, the peak of median percentage of stat5-p inhibition appeared [4].
Enzyme inhibitor
This orally bioavailable JAK inhibitor and anti-rheumatoid arthritis drug (FW = 326.39 g/mol; CAS 944118-01-8; Solubility: 200 mM in DMSO), also named ASP015K, JNJ-54781532, and trans-4-[[5-hydroxy-2- adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, targets Janus Kinase JAK1, JAK2, JAK3 and the nonreceptor tyrosine kinase Tyk2 enzyme with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM, respectively. Itsselectively suppress JAK3 or JAK1/2, respectively, may explain the weaker effects on red blood cells and platelets reported to be caused by JAK2 inhibition. Moreover, peficitinib improves symptoms in RA animal models after once-daily oral administration and demonstrates dosedependent improvement in psoriatic disease activities in a 6-week phase IIa study. The terminal mean half-life of peficitinib is 7–13 hours in pharmacological studies with healthy subjects
References
[1]. takeuchi t, tanaka y, iwasaki m, et al. efficacy and safety of the oral janus kinase inhibitor peficitinib (asp015k) monotherapy in patients with moderate to severe rheumatoid arthritis in japan: a 12-week, randomised, double-blind, placebo-controlled phase iib study. annals of the rheumatic diseases, 2015: annrheumdis-2015-208279.
[2]. digicaylioglu m, lipton sa. erythropoietin-mediated neuroprotection involves cross-talk between jak2 and nf-κb signalling cascades. nature, 2001, 412(6847): 641-647.
[3]. yamazaki s, morio h, inami m, et al. thu0101 asp015k: a novel jak inhibitor demonstrated potent efficacy in adjuvant-induced arthritis model in rats. annals of the rheumatic diseases, 2013, 72(suppl 3): a197-a197.
[4]. zhu t, valluri u, lewand m, et al. thu0256 pharmacodynamics of asp015k, a novel janus kinase inhibitor, in healthy volunteers. annals of the rheumatic diseases, 2013, 72(suppl 3): a252-a252.
Peficitinib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Fuxin Pharmaceutical | +86-021-021-50872116 +8613122107989 | contact@fuxinpharm.com | China | 10297 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| Alfa Chemistry | +1-5166625404 | Info@alfa-chemistry.com | United States | 21317 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| RR Scientific LLC | +86-13917743231 | sales@rrscientific.com | United States | 878 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
View Lastest Price from Peficitinib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2019-12-27 | Peficitinib
944118-01-8
|
US $1.00 / KG | 1KG | 97%-99.9% | 100kg | Career Henan Chemical Co |
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- Peficitinib
944118-01-8
- US $1.00 / KG
- 97%-99.9%
- Career Henan Chemical Co