MS154 [CAS 2550393-21-8]

MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand ; black: linker (HY-W096167) ; pink: EGFR ligand (HY-168305) ).

[2550393-21-8]

C46H54ClFN8O8

901.42

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCCCCCCCCNC(CCN4CCN(CCCOC5=CC6=C(NC7=CC=C(C(Cl)=C7)F)N=CN=C6C=C5OC)CC4)=O)=CC=C3)=O)=O

EGFR; PROTACs

Cereblon; EGFR/ErbB1/HER1

99.71

DMSO : 90.14 mg/mL (ultrasonic; warming)

-20°C, 3 years (Powder)

Blue Ice