ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3alpha by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells[1][2].
Molecular Weight:
528.53
Purity:
98.05
CAS Number:
[2089721-94-6]
Formula:
C25H27F3N8O2
Target:
EGFR,GSK-3,PD-1/PD-L1
Application Notes:
MCE Product type: Reference compound
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