MS9427 is a potent PROTAC EGFR degrader with K d s of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
性状
Solid
IC50 & Target[1][2]
EGFR (WT) 7.1 nM (Kd) EGFR L858R 4.3 nM (Kd)
体外研究(In Vitro)
MS9427 对 HCC-827 细胞具有抗增殖活性,GI50 为 0.87 ± 0.27 μM。MS9427 (0-10μM, 16 h) 有效诱导 EGFR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)。 has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 70 mg/mL (70.46 mM; Need ultrasonic)配制储备液