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JR-AB2-011
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JR-AB2-011图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

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 结合来抑制 mTORC2 活性(Ki:0.19 μM)。 JR-AB2-011 具有抗多形性胶质母细胞瘤 (GBM) 特性。
Canonical SMILESClC1=C(Cl)C=C(NC(N2/C(SC(C)C2)=N/C3=CC=C(F)C=C3)=O)C=C1
分子式C17H14Cl2FN3OS
分子量398.28
溶解度DMSO : 62.5 mg/mL (156.92 mM);Water :< 0.1 mg/mL (insoluble)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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]. mTORC2|0.36 μM (IC50)

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

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]

[1]. Benavides-Serrato A, et al. Specific blockade of Rictor-mTOR association inhibits mTORC2 activity and is cytotoxic in glioblastoma. PLoS One. 2017 Apr 28;12(4):e0176599.