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，Kd 分别为 1.3 nM、77 nM 和 6.5 nM。
货号:ajcx39634
CAS:2376136-61-5
分子式:C45H56ClN9O7
分子量：870.44
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

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)[1]. MS170 (10 nM-10 μM) effectively inhibits the proliferation in multiple cancer cell lines[1]. MS170 (1 nM-10 μM) concentration-dependently depletes cellular total AKT (T-AKT) with the DC50 value of 32±18 nM[1].

MS170 (a single intraperitoneal injection at a dose of 50 mg/kg) is bioavailable in mice via IP injection[1].

[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.