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Oclacitinib maleate

Catalog No. T6914   CAS 1640292-55-2
Synonyms: PF-03394197 maleate, PF-03394197

Oclacitinib maleate (PF-03394197 maleate) 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 Chemical Structure
Oclacitinib maleate, CAS 1640292-55-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 46.00
5 mg In stock $ 72.00
10 mg In stock $ 101.00
25 mg In stock $ 178.00
50 mg In stock $ 286.00
100 mg In stock $ 480.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 99.17%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Oclacitinib maleate (PF-03394197 maleate) 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: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 maleate, PF-03394197
Molecular Weight 453.51
Formula C15H23N5O2S·C4H4O4
CAS No. 1640292-55-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 15 mg/mL (33.1 mM)

Ethanol: 83 mg/mL (183 mM)

DMSO: 83 mg/mL (183 mM)

TargetMolReferences 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-Cancer Drug Library FDA-Approved Kinase Inhibitor Library Drug Repurposing Compound Library EMA Approved Drug Library Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Approved Drug Library Bioactive Compounds Library Max Anti-Prostate Cancer Compound Library

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Vidarabine Decernotinib NVP-BSK805 Cerdulatinib hydrochloride Ruxolitinib Hypericin AZ7550 BMS-911543

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Keywords

Oclacitinib maleate 1640292-55-2 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Oclacitinib PF 03394197 PF-03394197 maleate PF-03394197 Maleate inhibit PF03394197 Maleate PF03394197 Oclacitinib Maleate Inhibitor PF 03394197 Maleate PF-03394197 Janus kinase inhibitor

 

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