| Identification | Back Directory | [Name]
Mutated EGFR-IN-3 | [CAS]
2375107-27-8 | [Synonyms]
11H-Dibenzo[b,e][1,4]diazepin-11-one, 8-fluoro-5,10-dihydro-2-[4-(4-methyl-1-piperazinyl)phenoxy]-10-(phenylmethyl)- | [Molecular Formula]
C31H29FN4O2 | [MDL Number]
MFCD32671352 | [MOL File]
2375107-27-8.mol | [Molecular Weight]
508.59 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
EGFRL858R/T790M: 12 nM (IC50); EGFRC797S: 13 nM (IC50) | [References]
[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. DOI:10.1021/acsmedchemlett.9b00381 |
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