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编 号:F751679
分子式:C58H81ClN10O7S
分子量:1097.84
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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.

体内研究:
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.Animal Model:Male Swiss albino mice
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.

体外研究:
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). MS98 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines. MS98 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC50 value of 78±64 nM.
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