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编 号:F751676
分子式:C45H56ClN9O7
分子量:870.44
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1mg
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生物活性:
MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively.

体内研究:
MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection.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 is1.4 μM at 2 h.

体外研究:
Cereblon (CRBN)-recruiting degrader MS170 is an effective AKT degrader without a ″hook effect″. MS170 selectively induces robust AKT protein degradation, inhibits downstream signaling, and suppresses cancer cell proliferation. MS170 concentration- and time-dependently induces AKT degradation through the ubiquitin-proteasome system (UPS). MS170 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines. MS170 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC50 value of 32±18 nM.
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