化合物JR-AB2-011 T11728

Product Introduction
Bioactivity


英文名: JR-AB2-011

描述: JR-AB2-011 是一种选择性 mTORC2抑制剂，IC50值为 0.36 μM。JR-AB2-011 通过阻断 Rictor-mTOR 联合体 (Ki: 0.19 μM) 抑制 mTORC2 活性，并且具有抗多形性胶质母细胞瘤 (GBM) 的活性。

体外活性: JR-AB2-011 (1 μM; 24 hours) shows good anti-GBM properties, blocks mTORC2 signaling and Rictor association with mTOR [1]. JR-AB2-011 (0.5-2 μM; 48 hours) displays the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM compared to CID613034 [1]. Apoptosis Analysis [1] Cell Line: U87 GBM cells; LN229 GBM cells Concentration: 1 μM Incubation Time: 24 hours Result: Had good anti-GBM properties and blocked mTORC2 signaling and Rictor association with mTOR. Cell Cytotoxicity Assay [1] Cell Line: Normal mature human neurons Concentration: 0.5, 1, 2 μM Incubation Time: 48 hours Result: Displayed the least toxicity to normal neurons with no significant cytotoxic effects for concentrations up to 10 mM.

体内活性: Mice receiving JR-AB2-011 (4 mg/kg; daily i.p. for 10 days; 20 mg/kg; daily i.p. for 10 days) at either dosing regimen show significant inhibition of tumor growth rate (JR-AB2-011 at 4 mg/kg/d; 74% inhibition at end of dosing period; tumor growth delay 10.0 days; JR-AB2-011 at 20 mg/kg/d; 80% inhibition at end of dosing period; tumor growth delay 12.0 days) as compared to mice receiving vehicle alone [1]. Animal Model: LN229 cells in female C.B.-17-scid (Taconic) mice [1] Dosage: 4 mg/kg; 20 mg/kg Administration: Daily i.p.; 10 days Result: Either dosing regimen displayed marked inhibition of tumor growth rate as compared to mice receiving vehicle alone.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 61.5 mg/mL(154.41 mM)


关键字: JRAB2011 | JR-AB2-011 | JR-AB-2-011 | JR AB2 011

相关产品: mTOR inhibitor 9e | PI3Kα/mTOR-IN-1 | Arnicolide D | KU-0063794 | GSK-25 | PI3K/Akt/mTOR-IN-2 | GNE-317 | Torin 2 | ETP-46464 | Cbz-B3A

相关库: Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Pyroptosis Compound Library | Oxidation-Reduction Compound Library | Glutamine Metabolism Compound Library | Kinase Inhibitor Library | Inhibitor Library | Reprogramming Compound Library | Glycolysis Compound Library | Bioactive Compound Library

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