egfrin12

EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

EGFR-IN-127 is an ATP-competitive inhibitor targeting EGFR, with IC50 values of 136.3 nM for EGFRdel19 and 161.2 nM for EGFRdel19/T790M/C797S. This compound holds potential for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-124 (compound 10A) is an EGFR inhibitor with an IC50 value of 0.54 μM, utilized in cancer research.

EGFR-IN-129 (Compound 10b) is an effective, selective EGFR inhibitor with an IC50 of 51.2 nM and demonstrates broad-spectrum antiproliferative activity against the NCI tumor panel.

EGFR-IN-128 (compound 28) is a potent and selective molecule targeting wild-type EGFREx20Ins, demonstrating therapeutic efficacy across various human xenograft models and capable of penetrating the blood-brain barrier in preclinical species.

EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM for EGFR(d746-750/T790M/C797S), 0.52 nM for EGFR(L858R/T790M/C797S), 0.5 nM for EGFR(d746-750/C797S), 0.69 nM for EGFR(L858R/C797S), and 0.92 nM for EGFR (wild type).

EGFR-IN-120 (Compound 11eg) is an orally effective EGFR inhibitor. It exhibits potency against the EGFR L858R/T790M/C797S mutant with an IC50 of 0.053 μM, and displays weaker activity against EGFRWT, with an IC50 of 1.05 μM. EGFR-IN-120 inhibits the phosphorylation of EGFR as well as key downstream effectors including STAT3, AKT, and Erk. This compound induces cell cycle arrest and apoptosis in cells harboring the EGFR mutation. Additionally, EGFR-IN-120 inhibits the proliferation of NSCLC cells containing the EGFR L858R/T790M/C797S mutation, with an IC50 value of 0.052 μM.

EGFR-IN-121 (compound 15) acts as a dual inhibitor for EGFR and VEGFR-2, with IC50 values of 84 nM and 3.5 nM, respectively.