| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: =99.85%
Dp44mT is a novel and potent iron chelator with DNA-damaging activity mediated by top2a inhibition and with selective antitumor activity. In the human breast cancer cell line MDA-MB-231, Dp44mT specifically inhibits topoisomerase IIα, with a GI50 value of ~100 nmol/L. In comparison to wild type cells, Nalm-6 leukemic top2α+/- cells expressed ~57% more top2α enzyme in control experiments. Comparatively to top2α+/+ cells, treated with Dp44mT at 100 nmol/L, top2α+/- cells displayed partial resistance to the drug's cytotoxic effects. The top2α+/+ cells displayed 31.7% sub-G1 containing cells following exposure to Dp44mT at 100 nmol/L, compared to the top2α+/- cells' 9.4%.
| Targets |
Iron chelator
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| ln Vitro |
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. In SK-N-MC neuroepithelioma and M109 cells, Dp44mT reduces the amount of Fe that cells take up from Fe-Tf and triggers cell apoptosis. [1] When topoisomerase topo2 is specifically targeted by Dp44mT in MDA-MB-231 cells, DNA damage results. [2] By stealing control of lysosomal P-glycoprotein (Pgp), Dp44mT, a Pgp substrate, also defeats multidrug resistance. [3]
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| ln Vivo |
Dp44mT (0.4 mg/kg, i.v.) inhibits tumor growth in CD2F1 mice carrying M109 tumors in a dose-dependent manner. [1]
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| Enzyme Assay |
For DNA topoisomerase II assays, the 5' ends of single stranded oligonucleotides or the 161-bp fragment from pBluescript SK(-) phagemid DNA are labeled with [32P]ATP and T4 polynucleotide kinase. To remove the unincorporated label, labeling mixtures are then centrifuged through Mini Quick Spin DNA columns (for pSK fragments) or Oligo columns (for oligonucleotides). The reaction mixture is heated to 95 °C and overnight cooled to room temperature in 10 mM Tris-HCl (pH 7.8), 100 mM NaCl, and 1 mM EDTA before being annealed to the complementary strand of the oligonucleotides. DNA substrates (10 pmol/reaction) are incubated with 500 ng of top2a or top2h in 10 L of reaction buffer at 25°C for the indicated times in the presence or absence of Dp44mT. SDS (final concentration of 0.5%) is added to stop reactions. Samples are separated on polyacrylamide denaturing gels at 16% (for pSK DNA) or 20% (for oligonucleotides) denaturing concentrations (7 M urea). A PhosphorImager[1] is used for imaging and quantitation.
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| Cell Assay |
DFO, 311, 3-aminopyridine-2-carboxaldehyde thiosemicarbazone, doxorubicin, and the DpT series of chelators (0-25 μM) are incubated with and without the cells for 72 hours at 37°C. Using the MTT assay, the chelators' impact on cell proliferation is investigated.
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| Animal Protocol |
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| References |
| Molecular Formula |
C14H15N5S
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| Molecular Weight |
285.37
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| Exact Mass |
285.10
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| Elemental Analysis |
C, 58.93; H, 5.30; N, 24.54; S, 11.23
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| CAS # |
152095-12-0
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| Appearance |
Solid powder
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| SMILES |
CN(C)C(=S)NN=C(C1=CC=CC=N1)C2=CC=CC=N2
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| InChi Key |
XOBIGRNRXCAMJQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H20N4O4S/c1-30-24-26-23(16-7-12-20-21(13-16)32-15-31-20)28(27-24)18-10-8-17(9-11-18)25-22(29)14-33-19-5-3-2-4-6-19/h2-13H,14-15H2,1H3,(H,25,29)
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| Chemical Name |
3-(dipyridin-2-ylmethylideneamino)-1,1-dimethylthiourea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: Propylene glycol : 1 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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