A2AR/EGFR-IN-1 

A2AR/EGFR-IN-1 is a dual A2AR/EGFR inhibitor, with an IC₅₀ of 0.037 μM against A2AR and an IC₅₀ of 8.37 μM against EGFR. A2AR/EGFR-IN-1 induces cell cycle arrest at S and G2/M phases. A2AR/EGFR-IN-1 upregulates the expression of TP53, Caspase3 and Bax, downregulates the expression of Bcl2, and promotes cell Apoptosis. A2AR/EGFR-IN-1 restores colon crypt structure in an azoxymethane (HY-111375)-induced colorectal cancer model in vivo. A2AR/EGFR-IN-1 can be used for research related to colorectal cancer^[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.

A2AR/EGFR-IN-1 (0.1 mg/kg; i.p.; once every three days; 2 weeks) restores the colonic crypt structure and controls precancerous lesions in azoxymethane (HY-111375)-induced colorectal cancer rats^[1].

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

484.83

C₂₄H₁₆Cl₃N₃S

ClC1=C(C2CC(C3=CC=CC=C3)=NN2C4=NC(C5=CC=C(Cl)C=C5)=CS4)C(Cl)=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Elzoghbi NZ, et al. Development of dual A2AR/EGFR targeting pyrazoline-thiazole hybrids for restored apoptotic balance in colorectal cancer. Bioorg Chem. 2026;179:109985.