Dp44mT是一种具有选择性抗癌活性的铁螯合剂。

Dp44mT, a effective iron chelator, has selective antitumor activity.

In MDA-MB-231 cells, Dp44mT selectively targets towards topoisomerase topo2α resulting in DNA damage. Dp44mT inhibits antiproliferative effects significantly with IC50 of 30 nM, 60 nM, and 60 nM for SK-N-MC, SK-Mel-28, and MCF-7 cells, respectively, while showing no effects on normal MRC-5 fibroblasts. In SK-N-MC neuroepithelioma and M109 cells,Dp44mT inhibits cellular Fe uptake from Fe-Tf , and induces cell apoptosis. Dp44mT, as a Pgp substrate, also overcomes multidrug resistance by the hijacking of lysosomal P-glycoprotein (Pgp).

Dp44mT (0.4 mg/kg, i.v.) inhibits M109 tumor implanted in CD2F1 mice by a dose-dependent manner.

SK-N-MC, SK-Mel-28, MCF-7 and MRC-5 cells are incubated in the presence and absence of DFO, 311, 3-aminopyridine-2-carboxaldehyde thiosemicarbazone, doxorubicin, and the DpT series of chelators (0-25 μM) for 72 hours at 37°C. The effect of the chelators on proliferation is examined using the MTT assay.

CD2F1 mice that are implanted M109 tumors intravenous inject Dp44mT (dissolved in Propylene glycol) 4 mg/kg in twice daily.

152095-12-0

C14H15N5S

285.37

2-(二-2-吡啶基亚甲基)-N,N-二甲基肼基硫代甲酰胺

Ethanol:47 mg/mL (164.69 mM)
DMSO:57 mg/mL (199.74 mM)
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years