JR-AB2-011

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

JR-AB2-011  纯度: 98.53%

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。

JR-AB2-011

JR-AB2-011 Chemical Structure

CAS No. : 2411853-34-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2860 In-stock
5 mg ¥2600 In-stock
10 mg ¥4400 In-stock
25 mg ¥9400 In-stock
50 mg ¥16000 In-stock
100 mg ¥26000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JR-AB2-011 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • PI3K/Akt/mTOR Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Antioxidants Compound Library
  • Differentiation Inducing Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Angiogenesis Related Compound Library
  • Glucose Metabolism Compound Library
  • Targeted Diversity Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

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 (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties[1].

IC50 & Target[1]

mTORC2

0.36 μM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 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[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.

分子量

398.28

Formula

C17H14Cl2FN3OS

CAS 号

2411853-34-2

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
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Benavides-Serrato A, et al. Correction: Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxicin glioblastoma. PLoS One. 2019 Feb 6;14(2):e0212160.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务