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808750-39-2

中文名称 MENSACARCIN
英文名称 Mensacarcin
CAS 808750-39-2
分子式 C21H24O9
分子量 420.41
MOL 文件 808750-39-2.mol
808750-39-2 结构式 808750-39-2 结构式

基本信息

中文别名
化合物 T12003
英文别名
Mensacarcin
(1R,2S,3S,4S,4aS,9aS,10S)-1,2,3,4-Tetrahydro-1,3,4-trihydroxy-5,10-dimethoxy-2-methyl-3-[[(2R,3S)-3-methyloxiranyl]carbonyl]-4a,9a-epoxyanthracen-9(10)-one

物理化学性质

储存条件-20°C储存
溶解度DMSO: soluble,Methanol: soluble
形态固体
颜色白色至灰白色

常见问题列表

生物活性
Mensacarcin 是一种高度复杂的聚酮类化合物,在肿瘤细胞系中普遍具有强烈的抑制细胞生长的作用,并可能诱导黑色素瘤细胞的凋亡 (apoptosis)。Mensacarcin 靶向线粒体 (mitochondria),影响线粒体的能量代谢,激活 caspase 依赖的凋亡途径。Mensacarcin 是一种抗生素,也可作为抗体偶联药物 (ADCs) 的细胞毒性成分。
靶点

Traditional Cytotoxic Agents

体外研究

Mensacarcin (0-100 μM; 24 hours) exhibits general cytostatic but type-specific cytotoxic effects for melanoma cells.
Mensacarcin (2-50 μM; 15 hours) induces rapid apoptotic cell death in melanoma cells.
Mensacarcin exhibits potent cytostatic properties (mean of 50% growth inhibition=0.2 μM) in almost all cell lines of the National Cancer Institute (NCI)-60 cell line screen and relatively selective cytotoxicity against melanoma cells. Mensacarcin is a highly oxygenated polyketide that was first isolated from soil-dwelling Streptomyces bacteria. Mensacarcin impairs mitochondrial function in melanoma cells.

Cell Viability Assay

Cell Line: SK-Mel-28 and SK-Mel-5 melanoma cells, HCT-116 colon cancer cells
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 24 hours
Result: Induced concentration- and time-dependent cell death in the two tested melanoma cell lines. HCT-116 colon carcinoma cells were strongly inhibited.

Western Blot Analysis

Cell Line: SK-Mel-28, SK-Mel-5 cells
Concentration: 2, 10, 50 μM
Incubation Time: 15 hours
Result: Induced the formation of 89-kDa PARP-1 fragments as well as caspase-3 activation in SK-Mel-28 and SK-Mel-5 beginning between 6 and 15 h after exposure.
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