BC-LI-0186

製品コードE0488 バッチE048801

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₂H₂₇N₃O₄S

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.3mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 86 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.61mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro	BC-LI-0186 binds to the RagD interacting site of LRS, thereby inhibiting lysosomal localization of LRS and mTORC1 activity. This compound 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]

プロトコル(参考用のみ)

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
	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.
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.

参考

https://pubmed.ncbi.nlm.nih.gov/28963468/

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：

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

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。