MS170

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MS170

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。

CAS NO:

2376136-61-5

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议

产品介绍

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，K_d分别为 1.3 nM、77 nM 和 6.5 nM。

生物活性

MS170 is a potent and selectivePROTACAKTdegrader. MS170 depletes cellular totalAKT(T-AKT) with theDC₅₀value of 32 nM. MS170 binds toAKT1,AKT2, andAKT3withK_ds 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 DC₅₀value 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 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].

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_maxis1.4 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.