MS170

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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。

MS170 

MS170 是一种有效的选择性 PROTAC AKT 降解剂。MS170 消耗细胞总 AKT (T-AKT)，DC50 值为 32 nM。MS170 与 AKT1、AKT2 和 AKT3 结合，Kd 分别为 1.3 nM、77 nM 和 6.5 nM。

MS170

MS170 Chemical Structure

CAS No. : 2376136-61-5

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生物活性

MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively[1].

IC50 & Target

Akt1

1.3 nM (Kd)

Akt2

77 nM (Kd)

Akt3

6.5 nM (Kd)

CRBN-DDB1

 

体外研究
(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)[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 DC50 value of 32±18 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 GI50s 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.

体内研究
(In Vivo)

MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 Cmax is1.4 μM at 2 h.

分子量

870.44

Formula

C45H56ClN9O7
CAS 号

2376136-61-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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