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D-I03

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Catalog No. T10936Cas No. 688342-78-1
Alias DI03

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.

D-I03

D-I03

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Purity: 99.65%
Catalog No. T10936Alias DI03Cas No. 688342-78-1
D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$31In StockIn Stock
5 mg$70In StockIn Stock
10 mg$128In StockIn Stock
25 mg$263In StockIn Stock
50 mg$392In StockIn Stock
100 mg$575In StockIn Stock
200 mg$818In Stock-
1 mL x 10 mM (in DMSO)$77In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.65%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.
Targets&IC50
RAD52:25.8 µM (Ki), single-chain annealing (SSA):5 µM, D-loop:8 µM
In vitro
D-IO3 (0-10 μM; on Days 1 and 3; Capan-1 and UWB1.289 cells) treatment preferentially inhibited the growth of Capan-1 and UWB1.289 cells in a concentration-dependent manner . D-IO3 inhibited cisplatin-induced RAD52 foci formation in the BCR-ABL1-positive BRCA1-deficient 32Dcl3 mouse hematopoietic cell line expressing GFP-RAD52. In the presence of D-IO3 (2.5 μM), the proportion of cells with RAD52 lesions decreased from 38.7% to 171%; meanwhile, the proportion of cisplatin-treated cells without lesions increased from 48.4% to 71.9%. D-IO3 had no effect on cisplatin-induced RAD51 foci. Similarly, D-I03 alone (in BRCA1-deficient cells) induced neither RAD51 nor RAD52 lesions, indicating that D-I03 has low genotoxicity[1].
In vivo
D-IO3 (50 mg / kg / day; intraperitoneal injection; daily; 7 consecutive days; nu / nu mice) treatment can reduce the growth of BRCA1-deficient MDA-MB-436 tumors. Talazoparib puls D-I03 does not cause any obvious toxicity to normal tissues and organs, and does not affect the growth of BRCA1-positive tumors. Pharmacokinetic and toxicity studies have shown that the maximum tolerated dose of D-I03 is ≥50mg / kg and t1 / 2 is 23.4 hours, resulting in a maximum concentration in peripheral blood> 1μM[1].
SynonymsDI03
Chemical Properties
Molecular Weight428.64
FormulaC23H36N6S
Cas No.688342-78-1
SmilesCCN(CC)CCNC(=S)Nc1ccc2nc(cc(C)c2c1)N1CCN(CC)CC1
Relative Density.1.147 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (209.97 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.7 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3330 mL11.6648 mL23.3296 mL116.6480 mL
5 mM0.4666 mL2.3330 mL4.6659 mL23.3296 mL
10 mM0.2333 mL1.1665 mL2.3330 mL11.6648 mL
20 mM0.1166 mL0.5832 mL1.1665 mL5.8324 mL
50 mM0.0467 mL0.2333 mL0.4666 mL2.3330 mL
100 mM0.0233 mL0.1166 mL0.2333 mL1.1665 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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