| Bioactivity | MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer[1]. |
| Invitro | MS9427 TFA 对 HCC-827 细胞具有抗增殖活性，GI50 为 0.87 ± 0.27 μM [1] 。MS9427 TFA (0-10μM, 16 h) 有效诱导 EGFRdel19降解 (DC50=82 ± 73 nM)，并在 HCC-827 细胞中以浓度依赖的方式抑制EGFR磷酸化(p-EGFR)[1]。 Western Blot Analysis[1] Cell Line: |
| Name | MS9427 TFA |
| Formula | C50H59ClF4N8O14 |
| Molar Mass | 1107.50 |
| 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. Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J Med Chem. 2022 Jun 23;65(12):8416-8443. |