Dp44mT

Name: Dp44mT
Brand: MedChemExpress
SKU: HY-18973
Rating: 5.0 (4 reviews)

Cat. No.: HY-18973 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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Dp44mT is an iron chelator with selective anticancer activity.

For research use only. We do not sell to patients.

Dp44mT Chemical Structure

CAS No. : 152095-12-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE Dp44mT

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Biological Activity
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Description

Dp44mT is an iron chelator with selective anticancer activity.

IC₅₀ & Target

Target: Iron chelator^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.02 μM Compound: Dp44mT	Antiproliferative activity at human A549 cells after 72 hrs by MTT assay Antiproliferative activity at human A549 cells after 72 hrs by MTT assay	[PMID: 22861499]
Capan-2	IC₅₀	0.001 μM Compound: 10; Dp44mT	Cytotoxicity against human Capan2 cells incubated for 24 hrs by MTT assay Cytotoxicity against human Capan2 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
CFPAC-1	IC₅₀	0.2 μM Compound: 10; Dp44mT	Cytotoxicity against human CFPAC-1 cells incubated for 24 hrs by MTT assay Cytotoxicity against human CFPAC-1 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
DMS-53	IC₅₀	0.01 μM Compound: Dp44mT	Antiproliferative activity at human DMS53 cells after 72 hrs by MTT assay Antiproliferative activity at human DMS53 cells after 72 hrs by MTT assay	[PMID: 22861499]
HCT-116	IC₅₀	0.0011 μM Compound: 1a; Dp44mT	Antiproliferative activity against human HCT116 cells deficient in p53 incubated for 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells deficient in p53 incubated for 72 hrs by MTS assay	[PMID: 30921758]
HCT-116	IC₅₀	0.00123 μM Compound: 1a; Dp44mT	Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay	[PMID: 30921758]
HCT-116	IC₅₀	0.002 μM Compound: Dp44mT	Antiproliferative activity against human HCT116 cells expressing p53 after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells expressing p53 after 72 hrs by MTT assay	[PMID: 22858101]
HCT-116	IC₅₀	0.005 μM Compound: Dp44mT	Antiproliferative activity against p53-deficient human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against p53-deficient human HCT116 cells after 72 hrs by MTT assay	[PMID: 22858101]
HL-60	IC₅₀	0.01 μM Compound: HDp44mT	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 19090766]
Hs 683	IC₅₀	0.00396 μM Compound: 1a; Dp44mT	Antiproliferative activity against human Hs683 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human Hs683 cells incubated for 72 hrs by MTS assay	[PMID: 30921758]
K562	IC₅₀	3.43 μM Compound: Dp44mT	Antiproliferative activity against human K562 cells by MTT assay Antiproliferative activity against human K562 cells by MTT assay	[PMID: 33132117]
K562/A02	IC₅₀	3.02 μM Compound: Dp44mT	Antiproliferative activity against human K562/A02 cells overexpressing P-gp by MTT assay Antiproliferative activity against human K562/A02 cells overexpressing P-gp by MTT assay	[PMID: 33132117]
KB 3-1	IC₅₀	0.07 μM Compound: Dp44mT	Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay	[PMID: 27336684]
MCF7	IC₅₀	0.00114 μM Compound: 1a; Dp44mT	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTS assay	[PMID: 30921758]
MIA PaCa-2	IC₅₀	0.001 μM Compound: 10; Dp44mT	Cytotoxicity against human MIAPaCa2 cells incubated for 24 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
MRC5	IC₅₀	> 10 μM Compound: Dp44mT	Antiproliferative activity at human MRC5 cells after 72 hrs by MTT assay Antiproliferative activity at human MRC5 cells after 72 hrs by MTT assay	[PMID: 22861499]
NHDF	IC₅₀	15.38 μM Compound: Dp44mT	Antiproliferative activity against human NHDF cells after 72 hrs by MTT assay Antiproliferative activity against human NHDF cells after 72 hrs by MTT assay	[PMID: 22858101]
NHDF	IC₅₀	18.88 μM Compound: 1a; Dp44mT	Antiproliferative activity against human NHDF cells incubated for 72 hrs by MTS assay Antiproliferative activity against human NHDF cells incubated for 72 hrs by MTS assay	[PMID: 30921758]
PANC-1	IC₅₀	0.004 μM Compound: 10; Dp44mT	Cytotoxicity against human PANC1 cells incubated for 24 hrs by MTT assay Cytotoxicity against human PANC1 cells incubated for 24 hrs by MTT assay	[PMID: 30904782]
SK-N-MC	IC₅₀	0.001 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 17602603]
SK-N-MC	IC₅₀	0.002 μM Compound: HDp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 19216562]
SK-N-MC	IC₅₀	0.002 μM Compound: HDp44mT	Antiproliferative activity against human SK-N-MC cells by MTT assay Antiproliferative activity against human SK-N-MC cells by MTT assay	[PMID: 17963372]
SK-N-MC	IC₅₀	0.004 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTS assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTS assay	[PMID: 21846118]
SK-N-MC	IC₅₀	0.004 μM Compound: Dp44mT	Antiproliferative activity at human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity at human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 22861499]
SK-N-MC	IC₅₀	0.004 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells measured after 72 hrs at 37 degC by MTT assay Antiproliferative activity against human SK-N-MC cells measured after 72 hrs at 37 degC by MTT assay	[PMID: 23312948]
SK-N-MC	IC₅₀	0.007 μM Compound: Dp44mT	Cytotoxicity against human SK-N-MC cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SK-N-MC cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23276209]
SK-N-MC	IC₅₀	0.01 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 22172311]
SK-N-MC	IC₅₀	0.01 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 21055950]
SK-N-MC	IC₅₀	0.01 μM Compound: HDp44mT	Antiproliferative activity against human SK-N-MC cells after 96 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 96 hrs by MTT assay	[PMID: 17064069]
SK-N-MC	IC₅₀	0.01 μM Compound: Dp44mT	Toxicity in human SK-N-MC cells by MTT method Toxicity in human SK-N-MC cells by MTT method	[PMID: 20041672]
SK-N-MC	IC₅₀	0.013 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 28841514]
SK-N-MC	IC₅₀	0.014 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 22858101]
SK-N-MC	IC₅₀	0.03 μM Compound: Dp44mT	Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay	[PMID: 19601577]
SW480	IC₅₀	0.06 μM Compound: Dp44mT	Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay	[PMID: 27336684]
SW480	IC₅₀	0.2 μM Compound: Dp44mT	Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay	[PMID: 27336684]
U-251	IC₅₀	0.00114 μM Compound: 1a; Dp44mT	Antiproliferative activity against human U251 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human U251 cells incubated for 72 hrs by MTS assay	[PMID: 30921758]
WI-38	IC₅₀	0.4 μM Compound: Dp44mT	Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay	[PMID: 27336684]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

285.37

Formula

C₁₄H₁₅N₅S

CAS No.

152095-12-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

S=C(N/N=C(C1=NC=CC=C1)\C2=NC=CC=C2)N(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (350.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (278 KB) SDS (479 KB)

COA (250 KB) HNMR (259 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

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]. MCE 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5042 mL	17.5211 mL	35.0422 mL	87.6056 mL
	5 mM	0.7008 mL	3.5042 mL	7.0084 mL	17.5211 mL
	10 mM	0.3504 mL	1.7521 mL	3.5042 mL	8.7606 mL
	15 mM	0.2336 mL	1.1681 mL	2.3361 mL	5.8404 mL
	20 mM	0.1752 mL	0.8761 mL	1.7521 mL	4.3803 mL
	25 mM	0.1402 mL	0.7008 mL	1.4017 mL	3.5042 mL
	30 mM	0.1168 mL	0.5840 mL	1.1681 mL	2.9202 mL
	40 mM	0.0876 mL	0.4380 mL	0.8761 mL	2.1901 mL
	50 mM	0.0701 mL	0.3504 mL	0.7008 mL	1.7521 mL
	60 mM	0.0584 mL	0.2920 mL	0.5840 mL	1.4601 mL
	80 mM	0.0438 mL	0.2190 mL	0.4380 mL	1.0951 mL
	100 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8761 mL

Dp44mT Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dp44mT152095-12-0ApoptosisFerroptosisInhibitorinhibitorinhibit

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Dp44mT

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Dp44mT Related Antibodies

4 Publications Citing Use of MCE Dp44mT

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Complete Stock Solution Preparation Table

Dp44mT Related Classifications

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