Oclacitinib maleate

Oclacitinib maleate (PF-03394197 maleate) 是一种新型JAK 抑制剂,有效抑制JAK1,IC50为 10 nM。

CAS号

1640292-55-2

分子式

C15H23N5O2S·C4H4O4

主要靶点

Tyrosine Kinases|JAK

仅限科研使用

Cat No : CM04902

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Synonyms

PF-03394197|PF-03394197 maleate|奥拉替尼马来酸盐



产品信息

Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.

CAS号 1640292-55-2
分子式 C15H23N5O2S·C4H4O4
主要靶点 Tyrosine Kinases|JAK
主要通路 JAK/STAT信号通路|干细胞|表观遗传|蛋白酪氨酸激酶|血管生成
分子量 453.51
纯度 99.17%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 PF-03394197|PF-03394197 maleate|奥拉替尼马来酸盐

靶点活性

JAK1-dependent:36 to 249 nM|JAK family members:10 to 99 nM

体内活性

PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7[2].

体外活性

PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells[1].

溶解度

DMSO:83 mg/mL (183 mM),Ethanol:83 mg/mL (183 mM),H2O:15 mg/mL (33.1 mM)

参考文献

1.Gonzales AJ, et al. J Vet Pharmacol Ther. 2014, 37(4):317-324.
2.Cosgrove SB, et al. Vet Dermatol. 2013, 24(5):479-e114.

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