ES-072 

ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α 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].

528.53

C₂₅H₂₇F₃N₈O₂

2089721-94-6

FC(F)(F)C1=C(NC2=CC=CC(NC(C=C)=O)=C2)N=C(NC3=CC=C(N4CCN(C)CC4)N=C3OC)N=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zheng J, et al. First-in-Human Phase 1 Study of ES-072, an Oral Mutant-Selective EGFR T790M Inhibitor, in Non-Small-Cell Lung Cancer. Clin Lung Cancer. 2020 Nov;21(6):509-519.e1.  [Content Brief]

  [2]. Wu Y, et al. ARIH1 signaling promotes anti-tumor immunity by targeting PD-L1 for proteasomal degradation. Nat Commun. 2021 Apr 20;12(1):2346.  [Content Brief]