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。
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. | ||||||||||||||||
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In Vitro | 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[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]. | ||||||||||||||||
Solvent & Solubility | In Vitro: 10 mM in DMSO Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. | ||||||||||||||||
References | |
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