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AG-1478 is an inhibitor of EGFR which acts on EGF-stimulated Erk1/2 phosphorylation with IC50 value of 10 uM using ovarian cell line Ishikawa [1].

EGFR (epidermal growth factor receptor) belongs to human HER-1 family, which is a cell surface receptor and recognized by EGF-family (epidermal growth factor family). Many studies have shown that EGFR is over-expressed in a variety of solid tumors and its over-expression means bad prognosis for cancer patients [1]. AG1478 works as EGFR kinase inhibitor through blocking EGFR phosphorylation and superoxide anion production [2].

Treating human hepatocellular carcinoma HA22T/VGH cells could reduce its anti-tumor activity compared with control group [3]. When tested with ovarian cancer cell lines CAOV-3 or SKOV-3, EGFR signaling was diminished [4]. When human colorectal SW480 was treated with AG-1478, both EGFR phosphorylation and cell proliferation were reduced [5].

In nu/nu mice model with CAOV-3 cells xenografted, treatment with AG-1478 could diminish EGFR phosphorylation thus limited the growth of tumor [4].

Gong XD, et al. had shown that AG-1478 also could reduce the expression of FOXM1 via FOXO3a using a NSCLC cell lines A549, and the A549 cells showed increased chemosensitivity[6].

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