Oclacitinib maleate

製品コードS8195 バッチS819501

印刷

化学情報

Chemical Structure Synonyms PF-03394197 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H23N5O2S.C4H4O4
分子量 453.51 CAS No. 1640292-55-2
Solubility (25°C)* 体外 DMSO 90 mg/mL (198.45 mM)
Ethanol 90 mg/mL (198.45 mM)
Water 18 mg/mL (39.69 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 Oclacitinib maleate (PF-03394197) 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. It does not inhibit a panel of 38 non-JAK kinases.
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].

プロトコル(参考用のみ)

キナーゼアッセイ Janus kinase enzyme activity assays and kinase selectivity panels
Recombinant human active kinase domains for JAK1, JAK2, JAK3, and TYK2 are used in isolated enzyme assays using Caliper microfluidics technology to determine potency of oclacitinib against the JAK family members. Sequence homology to the analogous sequences in the canine JAK enzymes are 98, 98, 100, and 90%, respectively. Invitrogen kinase panel testing is performed to determine potency of oclacitinib toward 38 different non-JAK kinases using their SelectScreen™ Kinase Profiling Services. Oclacitinib is evaluated at a concentration of 1 μM. Kinase-specific assay conditions and data analyses are described on Web site. This service utilizes the Z'-Lyte technology for all kinase screening. All tests were run in duplicate.
動物実験 動物モデル Dogs
投薬量 0.4–0.6 mg/kg
投与方法 orally twice daily

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A panel of janus kinase inhibitors identified with anti-inflammatory effects protect mice from lethal influenza virus infection [ Antimicrob Agents Chemother, 2024, 68(4):e0135023.] PubMed: 38470034
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Janus kinase inhibitors ruxolitinib and baricitinib impair glycoprotein-VI mediated platelet function [ Platelets, 2021, 1-12] PubMed: 34097573
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] PubMed: 31740922
A pharmacokinetic study of oclacitinib maleate in six cats. [ Vet Dermatol, 2020, 31(2):134-137] PubMed: 31769185

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。