产品说明书

Dp44mT

Print
Chemical Structure| 152095-12-0 同义名 : -
CAS号 : 152095-12-0
货号 : A548130
分子式 : C14H15N5S
纯度 : 99%+
分子量 : 285.367
MDL号 : MFCD20527329
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(367.95 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Dp44mT is an iron chelator with selective anticancer activity. Dp44mT alone induced selective cell killing in the breast cancer cell line MDA-MB-231, due to selective inhibition of top2alpha, 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 (gamma-H2AX) and Comet tails induced in MDA-MB-231 cells. Doxorubicin-induced cytotoxicity and DNA damage were both enhanced significantly in the presence of low concentrations of Dp44mT. The chelator caused selective poisoning of DNA topoisomerase IIalpha (top2alpha) as measured by an in vitro DNA cleavage assay and cellular topoisomerase-DNA complex formation[3]. 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[4]. Dp44mT induces translocation of TFEB to the nucleus and it was AMPK-dependent[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.50mL

0.70mL

0.35mL

17.52mL

3.50mL

1.75mL

35.04mL

7.01mL

3.50mL
参考文献

[1]Rao VA, Klein SR, 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]Yuan J, Lovejoy DB, et al. Novel di-2-pyridyl-derived iron chelators with marked and selective antitumor activity: in vitro and in vivo assessment. Blood. 2004 Sep 1;104(5):1450-8. Epub 2004 May 18.

[3]Rao VA, Klein SR, Agama KK, Toyoda E, Adachi N, Pommier Y, Shacter EB. 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

[4]Lovejoy DB, Jansson PJ, Brunk UT, Wong J, Ponka P, Richardson DR. 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

[5]Krishan S, Sahni S, Richardson DR. The anti-tumor agent, Dp44mT, promotes nuclear translocation of TFEB via inhibition of the AMPK-mTORC1 axis. Biochim Biophys Acta Mol Basis Dis. 2020 Dec 1;1866(12):165970