ES-072 - CAS 2089721-94-6

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.

GSK-3, EGFR, PD-1/PD-L1

Angiogenesis, Stem Cells, Apoptosis, PI3K/Akt/mTOR signaling, Tyrosine Kinase/Adaptors, Cell Cycle/Checkpoint, JAK/STAT signaling, Immunology/Inflammation

2089621

C25H27F3N8O2

528.53

O=C(C=C)NC1=CC=CC(=C1)NC2=NC(=NC=C2C(F)(F)F)NC=3C=CC(=NC3OC)N4CCN(C)CC4

-20°C

Ice Packs

Small Compound