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MS170

产品编号 T39928 CAS 2376136-61-5

MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.

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MS170, CAS 2376136-61-5

规格	价格/CNY		货期	数量
5 mg	￥ 9,990		待询

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	MS170 is a highly effective and specific PROTAC AKT degrader compound that exhibits potent activity. It efficiently reduces the levels of total AKT (T-AKT) within cells, with a DC 50 value of 32 nM. Furthermore, MS170 demonstrates strong binding affinity towards AKT isoforms, specifically AKT1, AKT2, and AKT3, with respective dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM.
靶点活性	Akt3:6.5 nM (Kd), Akt2:77 nM (Kd), Akt1:1.3 nM (Kd)
体外活性	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)[1]. MS170 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines[1]. MS170 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC 50 value of 32±18 nM[1]. Cell Proliferation Assay[1]Cell 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 Analysis[1]Cell 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.
体内活性	MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection[1]. Animal Model: Male Swiss albino mice[1]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.

分子量	870.45
分子式	C45H56ClN9O7
CAS No.	2376136-61-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Yu X, et al. Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders. J Med Chem. 2021;64(24):18054-18081.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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