ES-072

• 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].

• UNSPSC :

  12352005

• Target :

  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

• Purity :

  98.05

• Solubility :

  DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

• 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 Formula :

  C25H27F3N8O2

• Molecular Weight :

  528.53

• References & Citations :

  [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. |[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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  GSK-3α

• CAS Number :

  [2089721-94-6]