GLUT1/EGFR-IN-1 

GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research^[1].

GLUT1/EGFR-IN-1 (compound H) showed outstanding antitumour activity in CNE1 and MDA-MB231 cells, with IC₅₀ values lower than 3 µmol/L, but activity was not obvious in CNE2 cells^[1].
GLUT1/EGFR-IN-1 (0-4 μM, 48 h) inhibits the expression of EGFR and p-EGFR in both CNE1 and MDA-MB231 cells^[1].
GLUT1/EGFR-IN-1 (0-4 μM, 48 h) induces apoptosis in CNE1 and MDA-MB231 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GLUT1/EGFR-IN-1 (compound H) (4-8 mg/kg, IP, for two weeks) inhibits the growth of the MDA-MB231-transplanted tumour cells in a nude mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

696.75

C₄₄H₃₂N₄O₅

2393787-80-7

O=C(C1=C2C=C(C=C1OCC3=CC=CC=C3)C(NC4=CC=C(C5=C4)N=CN=C5NC6=CC=C(C=C6)C)=O)C7=C(C=CC=C7C2=O)OCC8=CC=CC=C8

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• [1]. Wang C, et al. Targeted blocking of EGFR and GLUT1 by compound H reveals a new strategy for treatment of triple-negative breast cancer and nasopharyngeal carcinoma. Eur J Pharm Sci. 2024 Jul 1;198:106789.  [Content Brief]