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].

Product Specifications

CAS Number

[2375107-27-8]

UNSPSC

12352005

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mutated-egfr-in-3.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C31H29FN4O2

Molecular Weight

508.59

References & Citations

[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.