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编 号：F751680
分子式：C59H81ClN12O6S
分子量：1121.87
分子式：C59H81ClN12O6S
分子量：1121.87
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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.
体内研究：
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.Pharmacokinetic Parameters of MS143 in male Swiss Albino mice.IP (75 mg/kg)
Cmax (μM)7
Tmax (h)2
AUC0-12 (h·ng/mL)63600
Animal Model:Male immunocompromised NU/J mice (6 weeks old)
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).
体外研究：
MS143 (1 nM-10 μM; 24 hours) induces T-AKT degradation with a concentration-dependent manner in PC3 cells.MS143 (0.1-10 μM;14 days, replenish every 2 days) effectively inhibits colony formation in BT474 cells.MS143 (1 μM; 24 hours) promotes AKT degradation in an E3 ligase- and UPS-dependent manner.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).
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.
体内研究：
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.Pharmacokinetic Parameters of MS143 in male Swiss Albino mice.IP (75 mg/kg)
Cmax (μM)7
Tmax (h)2
AUC0-12 (h·ng/mL)63600
Animal Model:Male immunocompromised NU/J mice (6 weeks old)
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).
体外研究：
MS143 (1 nM-10 μM; 24 hours) induces T-AKT degradation with a concentration-dependent manner in PC3 cells.MS143 (0.1-10 μM;14 days, replenish every 2 days) effectively inhibits colony formation in BT474 cells.MS143 (1 μM; 24 hours) promotes AKT degradation in an E3 ligase- and UPS-dependent manner.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).
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