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。JR-AB2-011 具有抗多形性胶质母细胞瘤 (GBM) 的活性。
| 生物活性 | JR-AB2-011 is a selectivemTORC2inhibitor with anIC50value of 0.36 μM. JR-AB2-011 inhibitsmTORC2activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties[1]. |
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体外研究
(In Vitro) | JR-AB2-011 (1 μM; 24 hours) has 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. |
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体内研究
(In Vivo) | 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 display marked 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(156.92 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5108 mL | 12.5540 mL | 25.1080 mL | | 5 mM | 0.5022 mL | 2.5108 mL | 5.0216 mL | | 10 mM | 0.2511 mL | 1.2554 mL | 2.5108 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.22 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.22 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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