EGFR mutant-IN-1

• UNSPSC Description:

  EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM)[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/egfr-mutant-in-1.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C1C(C2=CC=CC(F)=C2Cl)=C(C)C3=CN=C(NC4=CC=C(N5CCN(C)CC5)C(C)=C4)N=C3N1[C@H]6CN(C(CC)=O)CCC6

• Molecular Weight:

  632.17

• References & Citations:

  [1]Shen J, et al. Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type SparingInhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFRL858R/T790M/C797S). J Med Chem. 2019 Aug 8;62(15):7302-7308.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  No Development Reported