EGFR-IN-34

EGFR-IN-34 is a low-toxicity, acrylamide derivative antitumor agent that is a potent inhibitor of EGFR. Among others, overexpression and mutation of the epidermal growth factor receptor (EGFR) has been shown to lead to uncontrolled cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 exhibits potential for research in EGFR mutation-related diseases.

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R T790M), and EGFR(L858R T790M C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

Afatinib impurity 11 is a byproduct of Afatinib, an irreversible EGFR family inhibitor with IC50 values of 0.5 nM, 0.4 nM, 10 nM, and 14 nM for EGFRwt, EGFRL858R, EGFRL858R T790M, and HER2, respectively[1].

CAY10717 is a multi-targeted kinase inhibitor that exhibits greater than 40% inhibition of 34 of 104 kinases in an enzymatic assay at a concentration of 100 nM. It has activity at multiple oncogenic kinases, with IC50 values less than 50 nM against wild-type EGFR and ABL and mutant ABLG250E, ABLY253F, ABLE255K, and B-RafV600E. CAY10717 is highly cytotoxic against a cancer cell panel that includes chemotherapy-sensitive and -resistant cell lines (EC50s = 0.4-158 nM). It also inhibits the growth of human umbilical vein endothelial cells (HUVECs; EC50 = 34 nM), a model for tumor angiogenesis.

EGFR HER2-IN-8 (compound 34) is an inhibitor of EGFR, HER2, and DHFR with IC50 values of 0.45 μM, 0.244 μM, and 5.669 μM, respectively. It demonstrates anticancer activity against several cancer cell lines, exhibiting a high safety profile and selectivity indices, making it useful for cancer research [1].

HER2-IN-14 (Compound 34) is a potent HER2 inhibitor with an IC50 of 18 nM and demonstrates inhibitory activity against wild-type EGFR (wt-EGFR) with an IC50 of 6.3 μM [1].

Antiproliferative Agent-34 (Compound A14), a multitarget kinase inhibitor, demonstrates IC50 values of 177 nM for EGFR L858R T790M and 1567 nM for EGFR WT. Additionally, it inhibits JAK2, ROS1, FLT3, FLT4, and PDGFRα with respective IC50s of 30.93 nM, 106.90 nM, 108.00 nM, 226.60 nM, and 42.53 nM. In normoxic conditions, it suppresses the proliferation of H1975 and HCC827 cells with IC50 values below 40 nM, while under hypoxic conditions, its potency increases 4-6 fold, yielding IC50 values less than 10 nM [1].

EGFR-IN-90 (compound 34), an orally active EGFR inhibitor, demonstrates potent activity against EGFRL858R T790M C797S with an IC50 of 5.1 nM and effectively inhibits the proliferation of the H1975-TM cell line carrying EGFRL858R T790M C797S mutations with an IC50 of 0.05 μM. Additionally, EGFR-IN-90 suppresses tumor growth in the H1975-TM xenograft tumor model [1].