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152095-12-0

中文名稱 2-(二-2-吡啶基亞甲基)-N,N-二甲基肼基硫代甲酰胺
英文名稱 Iron Chelator, Dp44mT
CAS 152095-12-0
分子式 C14H15N5S
分子量 285.37
MOL 文件 152095-12-0.mol
更新日期 2024/12/18 10:22:08
152095-12-0 結(jié)構(gòu)式 152095-12-0 結(jié)構(gòu)式

基本信息

中文別名
2-(二-2-吡啶基亞甲基)-N,N-二甲基肼基硫代甲酰胺
英文別名
de44mt
Dp44mT
CS-2521
Iron Chelator
Iron Chelator, Dp44mT
Di-2-pyridylketone-4,4,-dimethyl-3-thiosemicarbazone
2-(Di-2-pyridinylmethylene)-N,N-dimethyl-hydrazinecarbothioamide
Hydrazinecarbothioamide, 2-(di-2-pyridinylmethylene)-N,N-dimethyl-
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件2-8°C
溶解度二甲基亞砜:≥5mg/mL
形態(tài)粉末
顏色黃色到橙色
敏感性感光
穩(wěn)定性Stable for 1 year from date of purchase as supplied. Solutions in DMSO may ne stored at -20°C for 1 month.

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
防范說明P301+P310
危險品標(biāo)志Xn
危險類別碼22
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3
危險等級6.1

常見問題列表

生物活性
Dp44mT是具有選擇性抗癌活性的鐵螯合劑 (iron chelator)。
靶點

Target: Iron chelator

體外研究

Dp44mT is cytotoxic to breast cancer cells, at least in part, due to selective inhibition of top2α. Dp44mT alone induced selective cell killing in the breast cancer cell line MDA-MB-231 when compared with healthy mammary epithelial cells (MCF-12A). It induces G1 cell cycle arrest and reduces cancer cell clonogenic growth at nanomolar concentrations. Dp44mT, but not the iron chelator desferal, induces DNA double-strand breaks quantified as S139 phosphorylated histone foci (γ-H2AX) and Comet tails induced in MDA-MB-231 cells. Doxorubicin-induced cytotoxicity and DNA damage are both enhanced significantly in the presence of low concentrations of Dp44mT. The chelator caused selective poisoning of DNA topoisomerase IIα (top2α) as measured by an in vitro DNA cleavage assay and cellular topoisomerase-DNA complex formation. Dp44mT targets lysosome integrity through copper binding. Copper binding is essential for the potent antitumor activity of Dp44mT, as coincubation with nontoxic copper chelators markedly attenuated its cytotoxicity.

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