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].

Product Specifications

CAS Number

[2089721-94-6]

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.