"目录号: HY-14808
Apoptosis-
Adarotene 是一种有效的apoptosis诱导剂，通过产生 DNA 损伤，来阻止人类肿瘤细胞的增殖。
Apoptosis
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生物活性
Description
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.
In Vitro
Adarotene causes a dose-dependent growth inhibition in a large panel of human tumor cell lines with IC50ranging 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[1]. 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[2].
In Vivo
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[1]. 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[2].
References
[1].Cincinelli R, et al. A novel atypical retinoid endowed with proapoptotic and antitumor activity. J Med Chem. 2003 Mar 13;46(6):909-12.
[2].Garattini E, et al. ST1926, a novel and orally active retinoid-related molecule inducing apoptosis in myeloid leukemia cells: modulation of intracellular calcium homeostasis. Blood. 2004 Jan 1;103(1):194-207.