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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EGFR/ErbB1/HER1
Curated Selection
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