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RBN-2397

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Catalog No. T12695Cas No. 2381037-82-5

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

RBN-2397

RBN-2397

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Purity: 99.8%
Catalog No. T12695Cas No. 2381037-82-5
RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$97In StockIn Stock
2 mg$142In StockIn Stock
5 mg$239In StockIn Stock
10 mg$388In StockIn Stock
25 mg$787In StockIn Stock
50 mg$987In StockIn Stock
100 mg$1,360In StockIn Stock
200 mg$1,830-In Stock
1 mL x 10 mM (in DMSO)$275In 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:99.8%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.
Targets&IC50
PARP7:1 nM (Kd), PARP7:3 nM (IC50)
In vitro
Inhibition of PARP7 with RBN-2397 can potently inhibit the growth of cancer cells and restore interferon signaling, effectively releasing the brake cancer uses to hide from the immune system and suppress both innate and adaptive immune mechanisms.RBN-2397 inhibits cells proliferation(IC50 value of 20 nM in NCI-H1373 lung cancer cells), shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells,and inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM[2].
In vivo
RBN-2397 oral administration induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.RBN-2397 oral administration causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg.The half-life (t1/2) of RBN-2397 in vivo is 325 mins[2].
Chemical Properties
Molecular Weight523.43
FormulaC20H23F6N7O3
Cas No.2381037-82-5
SmilesC[C@@H](COCCC(=O)N1CCN(CC1)c1ncc(cn1)C(F)(F)F)Nc1cn[nH]c(=O)c1C(F)(F)F
Relative Density.1.53 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (477.62 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.55 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 mM1.9105 mL9.5524 mL19.1048 mL95.5238 mL
5 mM0.3821 mL1.9105 mL3.8210 mL19.1048 mL
10 mM0.1910 mL0.9552 mL1.9105 mL9.5524 mL
20 mM0.0955 mL0.4776 mL0.9552 mL4.7762 mL
50 mM0.0382 mL0.1910 mL0.3821 mL1.9105 mL
100 mM0.0191 mL0.0955 mL0.1910 mL0.9552 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

Keywords

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