Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of theEGFR(L858R/T790M)andEGFR(L858R/T790M/C797S)mutants withIC₅₀values of 12 nM and 13 nM, respectively^[1].

Mutated EGFR-IN-3 inhibits EGFR through an allosteric mechanism, biochemical IC₅₀values 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].

508.59

C₃₁H₂₉FN₄O₂

2375107-27-8

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