产品说明书

Peficitinib

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Chemical Structure| 944118-01-8 同义名 : ASP015K;JNJ-54781532
CAS号 : 944118-01-8
货号 : A605997
分子式 : C18H22N4O2
纯度 : 98%
分子量 : 326.393
MDL号 : MFCD28502035
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(183.83 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • JAK2
描述 Peficitinb is an 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.32mL

3.06mL

1.53mL

30.64mL

6.13mL

3.06mL
参考文献

[1]Kivitz AJ, Gutierrez-Urena SR, et al. Peficitinib, a JAK Inhibitor, in the Treatment of Moderate-to-Severe Rheumatoid Arthritis in Patients With an Inadequate Response to Methotrexate. Arthritis Rheumatol. 2017 Apr;69(4):709-719.

[2]Takeuchi T, Tanaka Y, 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. Ann Rheum Dis. 2016 Jun;75(6):1057-64.