MS143

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MS143 

MS143 是一种有效的 AKT 降解剂，在 PC3 细胞中 DC50=46 nM，GI50=0.8 µM。MS143 通过劫持泛素-蛋白酶体系统，以浓度和时间依赖性的方式诱导快速、稳定的 AKT 降解。MS143 能抑制癌细胞生长。

MS143

MS143 Chemical Structure

CAS No. : 2376137-41-4

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生物活性

MS143 is a potent AKT degrader (DC50=46 nM and GI50=0.8 µM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth[1].

IC50 & Target

AKT
体外研究
(In Vitro)

MS143 (1 nM-10 μM; 24 hours) induces T-AKT degradation with a concentration-dependent manner in PC3 cells[1].
MS143 (0.1-10 µM;14 days, replenish every 2 days) effectively inhibits colony formation in BT474 cells[1].
MS143 (1 µM; 24 hours) promotes AKT degradation in an E3 ligase- and UPS-dependent manner[1].
MS143 (1 nM-10 µM) can inhibit the cell growth of PC3 cells (GI50=0.8 nM) and MDA-MB-468 cells (GI50=1.0 nM)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: PC3 cells and MDA-MB-468 cells[1]
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM
Incubation Time: 5 days
Result: Inhibited the cell growth of PC3 cells (GI50=0.8 nM) and MDA-MB-468 cells (GI50=1.0 nM).

Western Blot Analysis

Cell Line: PC3 cells[1]
Concentration: 1 μM
Incubation Time: 24 hours
Result: Promoted AKT degradation in an E3 ligase- and UPS-dependent manner.

体内研究
(In Vivo)

MS143 (75 mg/kg; i.p., 22 days) drastically inhibits the tumor growth by 92%, also substantially degrades T-AKT and P-AKT, and effectively inhibits the downstream signaling (PRAS40 phosphorylation) in xenograft mice[1].
Pharmacokinetic Parameters of MS143 in male Swiss Albino mice[1].

IP (75 mg/kg)
Cmax (μM) 7
Tmax (h) 2
AUC0-12 (h·ng/mL) 63600

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male immunocompromised NU/J mice (6 weeks old)[1]
Dosage: 75 mg/kg
Administration: i.p., 22 days
Result: Drastically inhibited the tumor growth by 92%, also substantially degraded T-AKT and P-AKT, and effectively inhibited the downstream signaling (PRAS40 phosphorylation).

分子量

1121.87

Formula

C59H81ClN12O6S
CAS 号

2376137-41-4
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. Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies. J Med Chem. 2022;65(4):3644-3666.

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