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化学情報
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Synonyms | BGB324 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C30H34N8 |
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| 分子量 | 506.64 | CAS No. | 1037624-75-1 | |
| Solubility (25°C)* | 体外 | DMSO | 11 mg/mL warmed with 50ºC water bath (21.71 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | ベムセンチニブ (Bemcentinib (R428、BGB324)) は Axl の阻害剤 (IC50 =14 nM) であり、Abl に比べて 100 倍以上の選択性を持ちます。 Mer および Tyro3 (50 ～ 100 倍) および InsR, EGFR, HER2および PDGFRβ に対しても高い Axl 選択性 (100 倍) を示します。 |
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| in vitro | R428 blocks the catalytic and procancerous activities of Axl. R428 inhibits Axl with low nanomolar activity and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. [1] In a recent study, the Axl inhibitor R428 shows a mean IC50 dose of ∼ 2.0μM for the primary CLL B cells after 24 hours of treatment and normal B-, T-, and natural killer (NK) cells show no significant amount of cell death at this dose of R428 (2.5 μM) under similar experimental conditions. [2] |
| in vivo | Pharmacologic investigations reveal favorable exposure after oral administration such that R428-treated tumors display a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibits angiogenesis in corneal micropocket and tumor models. R428 administration reduces metastatic burden and extends survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. [1] |
プロトコル(参考用のみ)
| キナーゼアッセイ | In vitro Kinase Assays | |
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| A five-point R428 dose titration is performed in radiometric in vitro kinase assays on 133 kinases at the KmATP for each kinase. Axl, Mer, and Tyro3 assays are also performed using a fluorescence polarization protocol. HER2 activity is determined by Z | ||
| 動物実験 | 動物モデル | MDA-MB-231-luc-D3H2LN Intracardiac Model |
| 投薬量 | 125 mg/kg | |
| 投与方法 | Oral, twice daily | |
参考
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カスタマーフィードバック
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Data from [Data independently produced by Cancer Res, 2014, 74(18), 5152-64]
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Data from [Data independently produced by Biochem Bioph Res Co, 2014, 10.1016/j.bbrc.2014.10.126]
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, , FASEB J, 2017, 31(4):1382-1397
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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。