For research use only. Not Intended for Therapeutic Use!
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AM580(Am-580; Ro 40-6055; NSC608001; CD336) is a stable retinobenzoic derivative originally synthesized as a RARα agonist.
Target: RARα agonist
in vitro: AM580 is a powerful inducer of granulocytic maturation in NB4, an APL-derived cell line, and in freshly isolated APL blasts. After treatment of APL cells with AM580 either alone or in combination with granulocyte colony-stimulating factor (G-CSF), the compound induces granulocytic maturation, as assessed by determination of the levels of leukocyte alkaline phosphatase, CD11b, CD33, and G-CSF receptor mRNA, at concentrations that are 10- to 100-fold lower than those of ATRA necessary to produce similar effects .
in vivo: A dose of 0.3mg/kg/day of Am580, was tested by treating 10 FVB mice for 4 months; no overt toxicity was found in liver, lungs, kidney, and spleen . 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. Immunocytochemical analysis showed that in these mice, RARα responsive genes such as Cyp26A1, E-cadherin, cellular retinol-binding protein 1 (CRBP1) and p27, were up-regulated .