EGFR-IN-136

EGFR-IN-136 (compound 21v) is a potent EGFR inhibitor with IC50 values of 20.2, 1.2, 2.3, 12.5 nM for EGFRWT, EGFRLR/TM, EGFR19D/TM/CS, EGFRLR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC[1].

Product Specifications

CAS Number

[3064450-12-7]

UNSPSC

12352005

Target

EGFR

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

COC1=CC(N2CCOCC2)=C(C3=CN4N=C3)C=C1NC5=NC(NC6=CC=C(OCCC4)C=C6P(C)(C)=O)=C(C)C=N5

Molecular Formula

C30H36N7O4P

Molecular Weight

589.63

References & Citations

[1]Hu S, et al. Design, Synthesis, and Biological Evaluation of Novel Diaminopyrimidine Macrocycles as Fourth Generation Reversible EGFR Inhibitors That Overcome Clinical Resistance to Osimertinib Mediated by C797S Mutation. J Med Chem. 2024 Nov 28;67 (22) :20531-20558.