GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of both GLUT1 and EGFR. It targets the ATP-binding site of the EGFR tyrosine kinase and inhibits GLUT1-mediated energy metabolism, resulting in reduced ATP, MMP, intracellular lactate, and nuclear translocation of EGFR. GLUT1/EGFR-IN-1 is applicable in the research of nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC).

GLUT1/EGFR-IN-1 (compound H) exhibits strong antitumor activity in CNE1 and MDA-MB231 cells with IC 50 values below 3 µmol/L, though its efficacy is less pronounced in CNE2 cells. In the presence of GLUT1/EGFR-IN-1 (0-4 μM, 48 hours), the expression of EGFR and p-EGFR is inhibited in both CNE1 and MDA-MB231 cells. Additionally, GLUT1/EGFR-IN-1 (0-4 μM, 48 hours) induces apoptosis in these cells.

Compound H (GLUT1/EGFR-IN-1) administered intraperitoneally (IP) at doses of 4-8 mg/kg over a period of two weeks inhibits the growth of MDA-MB231 transplanted tumor cells in a nude mouse model. This study utilized BALB/c-neu female mice, aged four to five weeks and numbering five in total, to examine the compound's efficacy.