JBJ-09-063 is a mutant-selective allosteric inhibitor targeting the epidermal growth factor receptor (EGFR). It exhibits potent inhibitory activity with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. JBJ-09-063 effectively attenuates phosphorylation of EGFR, Akt, and ERK1/2, demonstrating its utility in both TKI-sensitive and resistant models. This compound is particularly valuable for studying EGFR-mutant lung cancer and exploring therapeutic strategies for treatment-resistant variants.
JBJ-09-063 is a mutant-selective allosteric inhibitor targeting the epidermal growth factor receptor (EGFR). It exhibits potent inhibitory activity with IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S. JBJ-09-063 effectively attenuates phosphorylation of EGFR, Akt, and ERK1/2, demonstrating its utility in both TKI-sensitive and resistant models. This compound is particularly valuable for studying EGFR-mutant lung cancer and exploring therapeutic strategies for treatment-resistant variants.
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