AM580

Description: AM580 (also named CD336, NSC608001, Ro 40-6055) is a stable retinobenzoic analog that is originally synthesized as a novel, potent and selective RARalpha agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively. It is a powerful inducer of granulocytic maturation in NB4, an APL-derived cell line, and in freshly isolated APL blasts. In the presence of G-CSF, AM580 (at 10-8 M) produces a remarkable induction in LAP mRNA of NB4 cells. At a concentration of 10-5 M, AM580 and ATRA, in combination with G-CSF, induce almost the same level of LAP transcript. AM580 (at 10-8 M) leads to an approximately sixfold increase in the steady-state levels of the transcript coding for the G-CSF receptor in NB4 cells. The anticancer effect of RARalpha, together with the newly discovered pro-proliferative role of RARgamma, suggests that specific activation of RARalpha and inhibition of RARgamma might be effective in breast cancer therapy.

References: Blood. 1996 Feb 15; 87(4):1520-31; Oncogene. 2010 Jun 24; 29(25):3665-76.