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编 号：F618415
分子式：C31H29FN4O2
分子量：508.59
分子式：C31H29FN4O2
分子量：508.59
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CAS No: 2375107-27-8
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生物活性：
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.
体外研究：
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.Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 μM, 3.3 μM, 3.8μM, 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.Mutated EGFR-IN-3exhibits 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.
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.
体外研究：
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.Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 μM, 3.3 μM, 3.8μM, 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.Mutated EGFR-IN-3exhibits 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.
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