A2AR/EGFR-IN-1

A2AR/EGFR-IN-1 (Compound 6aii) (serial concentrations; 48 h) potently inhibits the viability of colorectal adenocarcinoma Caco2 cells with an IC₅₀ of 0.037 μM, while exerting no significant inhibitory effect on normal skin fibroblast (NHDF) cells^[1].
A2AR/EGFR-IN-1 is a dual inhibitor of EGFR (IC₅₀ = 8.37 μM) and A2AR (IC₅₀ = 0.037 μM)^[1].
A2AR/EGFR-IN-1 significantly reduces the cAMP expression level in Caco2 cells to 68.08 ng/mL, confirming its inhibitory effect on the downstream signaling pathway of A2AR^[1].
A2AR/EGFR-IN-1 induces apoptosis in 57.5% of Caco2 cells, increases the proportion of cells in the S phase to 57.5%, and reduces the proportion of cells in the G2/M phase by 30%^[1].
A2AR/EGFR-IN-1 restores the apoptotic balance in Caco2 cells by upregulating the pro-apoptotic proteins BAX, Caspase3 and TP53, and downregulating the anti-apoptotic protein Bcl2^[1].

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