| Bioactivity | MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively[1]. |
| Target | 798 nM (AKT-1), 90 nM (AKT-2), 544 nM (AKT-3) |
| Invitro | MS15 (0-10 μM，24 小时) TFA 可有效诱导 SW620 细胞和 MS21 抗性 KRAS/BRAF 突变细胞中的 AKT 降解[1]。MS15 (0-10 μM，5 天) TFA 抑制 KRAS 突变体 SW620 细胞的增殖[1]。MS15 (1 μM，1-24 小时) TFA 以时间和 UPS 依赖性方式介导 AKT 降解[1]。 0 --> MS15 TFA 相关抗体: |
| In Vivo | MS15 (75 mg/kg，腹腔注射，一次) 通过腹膜内给药在小鼠体内具有生物利用度[1]。 |
| Name | MS15 TFA |
| Formula | C66H80F3N11O7S |
| Molar Mass | 1228.47 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [1]. Yu X, et al. Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells. J Med Chem. 2022 Oct 27;65(20):14237-14260. |