计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
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文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC 50 value of 32 nM. MS170 binds to AKT1 , AKT2 , and AKT3 with K d s of 1.3 nM, 77 nM, and 6.5 nM, respectively
In Vitro
Cereblon (CRBN)-recruiting degrader MS170 is an effective AKT degrader without a ″hook effect″. MS170 selectively induces robust AKT protein degradation, inhibits downstream signaling, and suppresses cancer cell proliferation. MS170 concentration- and time-dependently induces AKT degradation through the ubiquitin-proteasome system (UPS). MS170 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines. MS170 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC 50 value of 32±18 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: BT474, PC3, and MDA-MB-468 cells Concentration: 10 nM, 100 nM, 1 μM, 10 μM Incubation Time: 5 days Result: Inhibited the cell growth with GI 50 s of 0.7±0.2 μM, 7.4±2.2 μM, and 5.7±2.4 μM for BT474 cells, PC3 cells, and MDA-MB-468 cells, respectively. Western Blot AnalysisCell Line: BT474 cells Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM , 3 μM, and 10 μM Incubation Time: 24 hours Result: Potently induced AKT degradation.
In Vivo
MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Swiss albino mice Dosage: Single 50 mg/kg(Pharmacokinetic Analysis) Administration: IP injection over 8 h Result: Bioavailable in mouse PK studies. The C max is1.4 μM at 2 h.
Form:Solid
IC50& Target:Akt1 1.3 nM (Kd) Akt2 77 nM (Kd) Akt3 6.5 nM (Kd) CRBN-DDB1
规格
规格或纯度
≥99%
英文名称
MS170
生化机理
MS170 是一种强效的选择性 PROTAC AKT 降解剂。MS170 降解细胞总 AKT（T-AKT）的 DC 50 值为 32 nM。MS170 与 AKT1、AKT2 和 AKT3 的结合 K d s 分别为 1.3 nM、77 nM 和 6.5 nM。
储存条件
避光,-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
870.44
技术文档
高级数据
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