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Synonyms | Storage (From the date of receipt) |
3 years -20°C powder | ||
化学式 | C22H27N3O4S |
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分子量 | 429.53 | CAS No. | 695207-56-8 | |
Solubility (25°C)* | 体外 | DMSO | 86 mg/mL (200.21 mM) | |
Water | Insoluble | |||
Ethanol | 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 | BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (LRS-RagD interaction) (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM), thereby inhibiting lysosomal localization of LRS and mTORC1 activity. It also effectively suppresses the activity of cancer-associated mTOR mutants and the growth of rapamycin-resistant cancer cells. |
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in vitro | BC-LI-0186 binds to the RagD interacting site of LRS, thereby inhibiting lysosomal localization of LRS and mTORC1 activity. BC-LI-0186 also effectively suppresses the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells.[1] |
in vivo | BC-LI-0186 (intraperitoneal injection; 50 mg/kg; alone or combines with cisplatin alone; 2 weeks; bid for 5 days per week) exhibits antitumor effects and significantly reduces tumor size compared with treatment with vehicle in an LSL K-ras G12D lung cancer animal model.[1] |
細胞アッセイ | 細胞株 | Human colon cancer cells, Human pancreatic cancer cells, Human breast cancer cells, Human ovary cancer cells, Human glioblastoma cells |
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濃度 | 0-20 μM | |
反応時間 | 15 min | |
実験の流れ | Cells are starved for 90 min in the leucine-free medium and then in the serum-free media for 15 min, or 1.5 h, or 6 h. And the cell lysates are analyzed with the corresponding antibodies. |
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動物実験 | 動物モデル | K-ras mouse lung cancer model, LSL K-ras G12D lung cancer mouse model |
投薬量 | 50 mg/kg | |
投与方法 | i.p. |
Combination of the LARS1 Inhibitor, BC-LI-0186 with a MEK1/2 Inhibitor Enhances the Anti-Tumor Effect in Non-Small Cell Lung Cancer [ Cancer Res Treat, 2023, 55(3):851-864] | PubMed: 36960627 |
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。