受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C18H20FN3O4 |
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分子量 | 361.37 | CAS No. | 1817626-54-2 | |
Solubility (25°C)* | 体外 | DMSO | 72 mg/mL (199.24 mM) | |
Ethanol | 3 mg/mL (8.3 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Zimlovisertib (PF-06650833) is a potent, selective inhibitor of IRAK4 with an IC50 of 0.2 nM. |
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in vitro | The kinome selectivity profile of PF-06650833 is assessed in a panel of 278 kinases(Invitrogen) at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4 while greater than 70% inhibition is observed for the following kinases, in order of potency: IRAK1, MNK2, LRRK2, CLK4, and CK1γ1. Lactam PF-06650833 is subsequently assessed in a whole cell functional VEGF2R assay (PAE-KDR cell line). No activity was observed at concentrations up to and including 30 µM. [1]. |
in vivo | PF-06650833 significantly inhibits LPS-induced TNF in a dose dependent manner. Mean exposures of PF-06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF-06650833 at 0.3 mg/kg, 1 mg/kg, 3 mg/kg and 30 mg/kg. The fraction unbound in rat plasma of PF-06650833 is 0.3.[1] |
動物実験 | 動物モデル | Male Sprague Dawley rats |
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投薬量 | 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg | |
投与方法 | Oral |
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] | PubMed: 35869064 |
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] | PubMed: 35869064 |
Pacritinib Inhibition of IRAK1 Blocks Aberrant TLR8 Signalling by SARS-CoV-2 and HIV-1-Derived RNA [ J Innate Immun, 2022, 1-11] | PubMed: 35785771 |
Inhibition of IRAK1/4 enhances the antitumor effect of lenvatinib in anaplastic thyroid cancer cells [ Cancer Sci, 2021, 112(11):4711-4721] | PubMed: 34328666 |
A temperature-regulated circuit for feeding behavior [ Research Square, 2021, 10.21203/rs.3.rs-916525/v1] | PubMed: None |
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。