product name Dp44mT
Description: Dp44mT is a potent iron chelator that shows selective antitumor activity. Dp44mT selectively inhibit topoisomerase IIα, with an GI50 value of ~100 nmol/L in the human breast cancer cell line MDA-MB-231. In control experiments, the Nalm-6 leukemic top2α+/- cells expressed ~57% as much levels of top2α enzyme as the wild type cells. Treated with Dp44mT at 100 nmol/L, compared with the top2α+/+ cells, top2α+/- cells showed partial resistance to the cytotoxic effects of the drug.After the exposure to Dp44mT at 100 nmol/L, the top2α+/+ cells showed 31.7%, while the top2α+/- cells only showed 9.4% sub-G1 containing cells.
References: Blood. 2004 Sep 1;104(5):1450-8; Cancer Res. 2009 Feb 1;69(3):948-57.
285.37
Formula
C14H15N5S
CAS No.
152095-12-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 57 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 47 mg/mL (164.7 mM)
Solubility (In vivo)
Propylene glycol: 1 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Dp44mT shows pronounced antiproliferative effects in SK-N-MC, SK-Mel-28, and MCF-7 cells with IC50 of 30 nM, 60 nM, and 60 nM, respectively, while no effects on normal MRC-5 fibroblasts. Dp44mT inhibits cellular Fe uptake from Fe-Tf in SK-N-MC neuroepithelioma and M109 cells, and induces cell apoptosis. In MDA-MB-231 cells, Dp44mT specifically targets topoisomerase topo2α, and thus causes DNA damage. Dp44mT, as a Pgp substrate, also overcomes multidrug resistance by the hijacking of lysosomal P-glycoprotein (Pgp). Kinase Assay: Cell Assay: Cells (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. |
|---|---|
| In Vivo | In CD2F1 mice bearing M109 tumors, Dp44mT (0.4 mg/kg, i.v.) inhibits tumor growth in a dose-dependent manner. |
| Animal model | CD2F1 mice bearing M109 tumors |
| Formulation & Dosage | Dissolved in Propylene glycol; 0.4 mg/kg, twice daily; i.v. injection |
| References | Blood. 2004 Sep 1;104(5):1450-8; Cancer Res. 2009 Feb 1;69(3):948-57. |
