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ES-072

CAT: 0931-T200087-01Size: 25 mgDry Ice: NoHazardous: No
CAT#:0931-T200087-01Size:25 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
2089721-94-6
Target
GSK-3|||EGFR|||PD-1/PD-L1
Related Pathways
Angiogenesis|||Stem Cells|||Apoptosis|||PI3K/Akt/mTOR signaling|||Tyrosine Kinase/Adaptors|||Cell Cycle/Checkpoint|||JAK/STAT signaling|||Immunology/Inflammation
Bioactivity
ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3?, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.
Smiles
O=C(C=C)NC1=CC=CC(=C1)NC2=NC(=NC=C2C(F)(F)F)NC=3C=CC(=NC3OC)N4CCN(C)CC4
Molecular Formula
C25H27F3N8O2
Molecular Weight
528.53
Shipping Conditions
Cool pack
Storage Temperature
-20°C

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