MS98

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MS98

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:

2376137-31-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

MS98 是一种有效的选择性PROTAC AKT降解剂。MS98 消耗细胞总AKT(T-AKT)，DC₅₀值为 78 nM。MS170 与 AKT1、AKT2 和 AKT3 结合，K_d分别为 4 nM，140 nM 和 8.1 nM。

生物活性

MS98 is a potent and selectivePROTACAKTdegrader. MS98 depletes cellular totalAKT(T-AKT) with theDC₅₀value of 78 nM. MS98 binds toAKT1,AKT2, andAKT3withK_ds of 4 nM, 140 nM, and 8.1 nM, respectively^[1].

IC₅₀& Target

Akt1

4 nM ()

Akt2

140 nM ()

Akt3

8.1 nM ()

VHL

体外研究
(In Vitro)

The von Hippel-Lindau (VHL)-recruiting degrader MS98 is an effective AKT degrader. MS98 selectively induces robust AKT protein degradation, inhibits downstream signaling, and suppresses cancer cell proliferation. MS98 concentration- and time-dependently induces AKT degradation through the ubiquitin-proteasome system (UPS)^[1].
MS98 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines^[1].
MS98 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC₅₀value of 78±64 nM^[1].

Cell Viability 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 1.3±0.3 μM, 9.2±1.3 μM, and 3.8±1.2 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)

MS98 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection. The maximum plasma concentration (C_max) reaches approximately 3.5 μM at 2 h, and the plasma concentrations remains above 3 μM over 8 h^[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_maxis 3.5 μM at 2 h.

分子量

1097.84

Formula

C₅₈H₈₁ClN₁₀O₇S

CAS 号

2376137-31-2

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.