ES-072

CAT: 0804-HY-164476-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-164476-01Size:5 mg
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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].
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.
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

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