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E7449

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Catalog No. T4471Cas No. 1140964-99-3
Alias UNII-9X5A2QIA7C, Stenoparib

E7449 (UNII-9X5A2QIA7C) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ~50 and ~50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.

E7449

E7449

😃Good
Purity: 97.13%
Catalog No. T4471Alias UNII-9X5A2QIA7C, StenoparibCas No. 1140964-99-3
E7449 (UNII-9X5A2QIA7C) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ~50 and ~50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$85In StockIn Stock
10 mg$123In StockIn Stock
25 mg$198In StockIn Stock
50 mg$298In StockIn Stock
100 mg$443In StockIn Stock
200 mg$655-In Stock
1 mL x 10 mM (in DMSO)$95In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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:97.13%
Appearance:solid
Color:White
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Product Introduction

Bioactivity
Description
E7449 (UNII-9X5A2QIA7C) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ~50 and ~50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate.
Targets&IC50
TNKS2:50 nM (IC50), PARP1:2 nM (IC50), PARP2:1 nM (IC50), TNKS1:50 nM (IC50)
In vitro
E7449 shows no obvious inhibiotry effects on PARP3 or PARPs 6-16. E7449 traps PARP1 onto damaged DNA, and affects DNA repair pathways beyond homologous recombination (HR). E7449 most potnetly suppresses cells deficient in components of the HR pathway (BRCA1 and 2, CtIP, Rad54). E7449 (10 μM) inhibits Wnt signaling in SW480 cells[1].
In vivo
E7449 moderately inhibits the growth of tumors at 100 mg/kg, and significantly ehhances the inhibition via 10, 30 and 100 mg/kg oral dosing in combination with temozolomide (TMZ) in the mouse melanoma B16-F10 isograft model[1].
SynonymsUNII-9X5A2QIA7C, Stenoparib
Chemical Properties
Molecular Weight317.34
FormulaC18H15N5O
Cas No.1140964-99-3
SmilesO=c1[nH][nH]c2nc(CN3Cc4ccccc4C3)nc3cccc1c23
Relative Density.1.53 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: 6.4 mg/mL (20.17 mM), Sonication and heating are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.1512 mL15.7560 mL31.5119 mL157.5597 mL
5 mM0.6302 mL3.1512 mL6.3024 mL31.5119 mL
10 mM0.3151 mL1.5756 mL3.1512 mL15.7560 mL
20 mM0.1576 mL0.7878 mL1.5756 mL7.8780 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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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