Mutated EGFR-IN-3 

Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC₅₀ values of 12 nM and 13 nM, respectively^[1].

Mutated EGFR-IN-3 inhibits EGFR through an allosteric mechanism, biochemical IC₅₀ values at varying ATP concentrations: 10 µM, 10.0 µM, 100.0 µM, 1000.0 µM are 15 nM, 8.3nM,11.0 nM and 8.3 nM, respectively for L858R/T790M cells^[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 µM, 3.3 µM, 3.8 µM, 4.0 µM and 4.5 µM for parental, WT, L858R, L858R/T790M and L858R/T790M/C797S, respectively in the absence of Cetuximab in Ba/F3 cells^[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 3.2 µM, 2.7 µM, 0.36 µM and 0.20 µM for WT,L858R, L858R/T790M and L858R/T790M/C797S, respectively in the presence of Cetuximab in Ba/F3 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

508.59

C₃₁H₂₉FN₄O₂

2375107-27-8

O=C1C2=CC(OC3=CC=C(N4CCN(C)CC4)C=C3)=CC=C2NC5=CC=C(F)C=C5N1CC6=CC=CC=C6

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• [1]. De Clercq DJH，et al. Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.ACS Med Chem Lett. 2019 Oct 22;10(11):1549-1553.  [Content Brief]