Mutated EGFR-IN-3

• UNSPSC Description:

  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].

• Target Antigen:

  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 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

• Clinical Information:

  No Development Reported

• CAS Number:

  2375107-27-8