ES-072 is a selective inhibitor of the EGFR-T790M mutation, primarily targeting this mutant receptor to activate GSK3α. By inhibiting EGFR-T790M activity, ES-072 promotes the phosphorylation of PD-L1 at Ser279 and Ser283, which facilitates its ubiquitination and subsequent proteasomal degradation via the E3 ligase ARIH1. This dual mechanism not only suppresses cancer cell proliferation but also enhances the anti-tumor immune response through reduced PD-L1 expression. ES-072 is applicable in research focused on non-small cell lung cancer (NSCLC) treatment strategies.
ES-072 is a selective inhibitor of the EGFR-T790M mutation, primarily targeting this mutant receptor to activate GSK3α. By inhibiting EGFR-T790M activity, ES-072 promotes the phosphorylation of PD-L1 at Ser279 and Ser283, which facilitates its ubiquitination and subsequent proteasomal degradation via the E3 ligase ARIH1. This dual mechanism not only suppresses cancer cell proliferation but also enhances the anti-tumor immune response through reduced PD-L1 expression. ES-072 is applicable in research focused on non-small cell lung cancer (NSCLC) treatment strategies.
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