ES-072

• UNSPSC Description:

  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].

• Target Antigen:

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

• Type:

  Reference compound

• Related Pathways:

  Immunology/Inflammation;JAK/STAT Signaling;PI3K/Akt/mTOR;Protein Tyrosine Kinase/RTK;Stem Cell/Wnt

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/es-072.html

• Smiles:

  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

• Molecular Weight:

  528.53

• References & Citations:

  [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.|[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.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported

• CAS Number:

  2089721-94-6