MS154

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 (HY-103596) ; black: linker (HY-W096167) ; pink: EGFR ligand (HY-168305) ) [1].

Product Specifications

CAS Number

[2550393-21-8]

UNSPSC

12352005

Target

EGFR; PROTACs

Type

Reference compound

Related Pathways

JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ms154.html

Purity

99.71

Solubility

DMSO : 90.14 mg/mL (ultrasonic; warming)

Smiles

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

Molecular Formula

C46H54ClFN8O8

Molecular Weight

901.42

References & Citations

[1]Meng Cheng, et al. Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders. J Med Chem. 2020 Feb 13;63 (3) :1216-1232.