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Oclacitinib maleate

Catalog No. T6914 CAS 1640292-55-2

Synonyms: PF-03394197, 奥拉替尼马来酸盐, PF-03394197 maleate

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.

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Oclacitinib maleate, CAS 1640292-55-2

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	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.
Targets&IC50	JAK1-dependent:36 to 249 nM, JAK family members:10 to 99 nM
In vitro	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].
In vivo	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].

Synonyms	PF-03394197, 奥拉替尼马来酸盐, PF-03394197 maleate
Molecular Weight	453.51
Formula	C19H27N5O6S
CAS No.	1640292-55-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 15 mg/mL (33.1 mM)

Ethanol: 83 mg/mL (183 mM)

DMSO: 83 mg/mL (183 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Stem Cell Differentiation Compound Library FDA-Approved & Pharmacopeia Drug Library Tyrosine Kinase Inhibitor Library

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Keywords

Oclacitinib maleate 1640292-55-2 JAK/STAT信号通路表观遗传蛋白酪氨酸激酶干细胞血管生成 Tyrosine Kinases JAK Oclacitinib PF03394197 inhibit PF 03394197 Inhibitor PF-03394197 PF-03394197 maleate Janus kinase inhibitor

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