MS170 是一种有效的选择性 PROTAC AKT 降解剂。MS170 消耗细胞总 AKT (T-AKT)，DC₅₀ 值为 32 nM。MS170 与 AKT1、AKT2 和 AKT3 结合，K_d 分别为 1.3 nM、77 nM 和 6.5 nM。

MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC 50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with K d s of 1.3 nM, 77 nM, and 6.5 nM, respectively.

Akt1 1.3 nM (Kd) Akt2 77 nM (Kd)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Swiss albino mice

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[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.