MS98

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MS98 

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，Kd 分别为 4 nM，140 nM 和 8.1 nM。

MS98

MS98 Chemical Structure

CAS No. : 2376137-31-2

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生物活性

MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds 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 DC50 value of 78±64 nM[1].

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

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 (Cmax) reaches approximately 3.5 μM at 2 h, and the plasma concentrations remains above 3 μM over 8 h[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 is 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.
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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