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Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation (ED50 = 0.79 nM) and apoptosis of HL-60 cells in vitro. Exhibits antiproliferative effects against a variety of human tumor cells lines (mean values of 35, 40 and 60% growth inhibition at 0.1, 1 and 10 ?M respectively) and displays anticancer activity against acute promyelocytic leukemia in vivo. It has also been shown to suppress the growth of other myeloid and lymphoid malignant cells.
B.A.Bernard; J.M.Bernardon; C.Delescluse; B.Martin; M.C.Lenoir; J.Maignan; B.Charpentier; W.R.Pilgrim; U.Reichert; B.Shroot. Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma. Biochem Biophys Res Commun. 1992, 186,(2), 977-983.
Shiro Jimi; Kota Mashima; Taichi Matsumoto; Shuji Hara; Junji Suzumiya; Kazuo Tamura. RARα is a regulatory factor for Am-80-induced cell growth inhibition of hematologic malignant cells. International Journal of Oncology. 2007, 31,(2), 397-404.