AM580 (CD336) is a retinoic acid receptor agonist that is selective for RARα( IC50 : 8 nM )

AM580 can inhibit the proliferation of various tumor cells,inhibiting survival signaling pathways and inducing apoptosis[1].

Modulation of the RARα/β to RARγ expression in mammary glands of normal mice, oncomice, and human mammary cell lines through the alteration of RAR-target gene expression affected cell proliferation, survival and tumor growth.?Treatment of MMTV-Myc mice with the RARα-selective agonist Am580 led to significant inhibition of mammary tumor growth (~90%, P<0.001), lung metastasis (P<0.01) and extended tumor latency in 63% of mice.?In these mice, RARα responsive genes such as Cyp26A1, E-cadherin, cellular retinol-binding protein 1 (CRBP1) and p27, were up-regulated[2].

Ishikawa cells were transfected with control siRNA or siRNA specific against the RARα gene.Cells were treated with vehicle control or AM580 for 18 h.Cells were stained with trypan blue and counted[1].

The effects of c-Myc on RAR isotype expression were evaluated in normal mouse mammary epithelium, mammary tumor cells obtained from the MMTV-Myc transgenic mouse model as well as human normal immortalized breast epithelial and breast cancer cell lines.?The in vivo effect of the RARα-selective agonist 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)carboxamido]benzoic acid (Am580) was examined in the MMTV-Myc mouse model of mammary tumorigenesis[2].