JR-AB2-011|cas:2411853-34-2|西域试剂

JR-AB2-011,98.53%

产品编号：Bellancom-122022| CAS NO：2411853-34-2| 分子式：C₁₇H₁₄Cl₂FN₃OS| 分子量：398.28

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货号	价格	库存与货期
Bellancom-122022	￥2600.00	杭州北京（现货）
Bellancom-122022	￥4400.00	杭州北京（现货）
Bellancom-122022	￥9400.00	杭州北京（现货）
Bellancom-122022	￥16000.00	杭州北京（现货）
Bellancom-122022	￥26000.00	杭州北京（现货）

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JR-AB2-011

产品介绍

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 (K_i: 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 selective mTORC2 inhibitor with an IC₅₀ value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (K_i: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.

体外研究

JR-AB2-011 (1 μM; 24 hours) has good anti-GBM properties, blocks mTORC2 signaling and Rictor association with mTOR.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

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

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	LN229 cells in female C.B.-17-scid (Taconic) mice
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	LN229 cells in female C.B.-17-scid (Taconic) mice
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	LN229 cells in female C.B.-17-scid (Taconic) mice
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (156.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
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。