Dp44mT

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Dp44mT  纯度: ≥98.0%

Dp44mT是具有选择性抗癌活性的铁螯合剂 (iron chelator)。

Dp44mT

Dp44mT Chemical Structure

CAS No. : 152095-12-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥660 In-stock
10 mg ¥600 In-stock
25 mg ¥1200 In-stock
50 mg ¥1900 In-stock
100 mg ¥2950 In-stock
200 mg   询价  
500 mg   询价  

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Dp44mT 相关产品

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生物活性

Dp44mT is an iron chelator with selective anticancer activity.

IC50 & Target

Target: Iron chelator[1]

体外研究
(In Vitro)

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[1]. 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[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

285.37

Formula

C14H15N5S

CAS 号

152095-12-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (350.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5042 mL 17.5211 mL 35.0422 mL
5 mM 0.7008 mL 3.5042 mL 7.0084 mL
10 mM 0.3504 mL 1.7521 mL 3.5042 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.76 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Rao VA, et al. The iron chelator Dp44mT causes DNA damage and selective inhibition of topoisomerase IIalpha in breast cancer cells. Cancer Res. 2009 Feb 1;69(3):948-57.

    [2]. Lovejoy DB, et al. Antitumor activity of metal-chelating compound Dp44mT is mediated by formation of a redox-active copper complex that accumulates in lysosomes. Cancer Res. 2011 Sep 1;71(17):5871-80.

Kinase Assay
[1]

For DNA topoisomerase IIα assays, the 161-bp fragment from pBluescript SK(-) phagemid DNA or single stranded oligonucleotides are 5′-end labeled with [32P]ATP and T4 polynucleotide kinase. Labeling mixtures are subsequently centrifuged through Mini Quick Spin DNA columns (for pSK fragments) or Oligo columns (for oligonucleotides) to remove the unincorporated label. Annealing to the complementary strand of the oligonucleotides is done by heating the reaction mixture to 95°C and overnight cooling to room temperature in 10 mM Tris-HCl (pH 7.8), 100 mM NaCl, and 1 mM EDTA. DNA substrates (10 pmol/reaction) are incubated with 500 ng of top2a or top2h in the presence or absence of Dp44mT for the indicated times at 25°C in 10 μL of reaction buffer. Reactions are stopped by adding SDS (final concentration 0.5%). Samples are separated on 16% (for pSK DNA) or 20% (for the oligonucleotides) denaturing polyacrylamide gels (7 M urea). Imaging and quantitation are done using a PhosphorImager[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cell proliferation is measured using a sulforhodamine B dye–based assay. MDA-MB-231(breast cancer) and MCF-12A (healthy mammary epithelial) cells are incubated with increasing concentrations of Dp44mT (0.01, 0.1, 1, 10, 100 μM). Results are expressed relative to control[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Rao VA, et al. The iron chelator Dp44mT causes DNA damage and selective inhibition of topoisomerase IIalpha in breast cancer cells. Cancer Res. 2009 Feb 1;69(3):948-57.

    [2]. Lovejoy DB, et al. Antitumor activity of metal-chelating compound Dp44mT is mediated by formation of a redox-active copper complex that accumulates in lysosomes. Cancer Res. 2011 Sep 1;71(17):5871-80.

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