| Identification | Back Directory | [Name]
2-Propenamide, N-[3-[[2-[[2-methoxy-6-(4-methyl-1-piperazinyl)-3-pyridinyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- | [CAS]
2089721-94-6 | [Synonyms]
2-Propenamide, N-[3-[[2-[[2-methoxy-6-(4-methyl-1-piperazinyl)-3-pyridinyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C25H27F3N8O2 | [MOL File]
2089721-94-6.mol | [Molecular Weight]
528.53 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
GSK-3α | [References]
[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. DOI:10.1016/j.cllc.2020.07.001
[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. DOI:10.1038/s41467-021-22467-8 |
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