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编 号:F369311
分子式:C25H26O3
分子量:374.47
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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生物活性:
Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.

体内研究:
Adarotene (15, 20 mg/kg, p.o.) causes a significant tumor growth inhibition in a human ovarian carcinoma, A2780/DX, and in a human melanoma, MeWo, growing in nude mice. Adarotene (30, 40 mg/kg, p.o.) results in a significant and dose-dependent increase in the life span of NB4-bearing SCID mice without overt toxicity.

体外研究:
Adarotene causes a dose-dependent growth inhibition in a large panel of human tumor cell lines with IC50 ranging from 0.1 to 0.3 μM. Adarotene causes cell accumulation in G1/S or S phase of cell cycle depending on tumor cells IGROV-1 and DU145. Adarotene is apoptotic and cytotoxic on a large spectrum of cancerous and leukemic cells, including freshly isolated AML blasts in primary culture. The molecular target of ST1926 apoptotic activity in myeloid leukemia cells is similar to the ligand-binding domain of RARγ. Adarotene treatment of cells results in rapid accumulation of intracellular calcium.
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