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808750-39-2

中文名稱 MENSACARCIN
英文名稱 Mensacarcin
CAS 808750-39-2
分子式 C21H24O9
分子量 420.41
MOL 文件 808750-39-2.mol
808750-39-2 結(jié)構(gòu)式 808750-39-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12003
英文別名
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

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: soluble,Methanol: soluble
形態(tài)固體
顏色白色至灰白色

常見問題列表

生物活性
Mensacarcin 是一種高度復(fù)雜的聚酮類化合物,在腫瘤細(xì)胞系中普遍具有強(qiáng)烈的抑制細(xì)胞生長的作用,并可能誘導(dǎo)黑色素瘤細(xì)胞的凋亡 (apoptosis)。Mensacarcin 靶向線粒體 (mitochondria),影響線粒體的能量代謝,激活 caspase 依賴的凋亡途徑。Mensacarcin 是一種抗生素,也可作為抗體偶聯(lián)藥物 (ADCs) 的細(xì)胞毒性成分。
靶點(diǎn)

Traditional Cytotoxic Agents

體外研究

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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