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BIBF0775

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Catalog No. T5197Cas No. 334951-90-5

BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).

BIBF0775

BIBF0775

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Purity: 99.79%
Catalog No. T5197Cas No. 334951-90-5
BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$36In StockIn Stock
5 mg$88In StockIn Stock
10 mg$137In StockIn Stock
25 mg$227In StockIn Stock
50 mg$319In StockIn Stock
100 mg$461-In Stock
200 mg$643-In Stock
1 mL x 10 mM (in DMSO)$97In 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:99.79%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM).
Targets&IC50
ALK5:34 nM
Kinase Assay
The inhibition of the kinase activity of TGFβRI was determined using the Promega Kinase-Glo kit according to the manufacturer's protocol in the presence of 600 nM ATP. N-terminally his-tagged human TGFβRI (aa 162-end) expressed in baculovirus and purified using nickel affinity chromatography was used at a final concentration of 0.03 μg/mL. The inhibition of the kinase activity of PDGFRR was determined using the Z0-LYTE assay technology according to the manufacturer's protocol. Full-length human PDGFRR (5.6 nM per assay) and the Tyr4 peptide (2 μM per assay) were obtained from Invitrogen, too. IC50 values were determined by the use of the Graph PadPrism software.
Cell Research
The high-content cytotoxicity assay (kit I) was performed according to the manufacturer's instructions. HaCaT cells were cultured overnight in black 96-well plates, incubated for 24 h with each compound at different concentrations, and stained with cytotoxicity cocktail. Cells were fixed, washed, and scanned on the Cellomics ArrayScan II platform. Images were analyzed with the Cell Health image analysis algorithm. Cytotoxicity indices were calculated for each of the four parameters (cellular membrane integrity, nuclear fragmentation and density, and lysosomal mass) to indicate the percentage of cells outside of the normal range which was defined using a vehicle-treated reference cell population.
Chemical Properties
Molecular Weight494.63
FormulaC31H34N4O2
Cas No.334951-90-5
SmilesCCN(C)C(=O)c1ccc2\C(=C(\Nc3ccc(CN4CCCCC4)cc3)c3ccccc3)C(=O)Nc2c1
Relative Density.1.223 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: 11 mg/mL (22.24 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.04 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 mM2.0217 mL10.1086 mL20.2171 mL101.0857 mL
5 mM0.4043 mL2.0217 mL4.0434 mL20.2171 mL
10 mM0.2022 mL1.0109 mL2.0217 mL10.1086 mL
20 mM0.1011 mL0.5054 mL1.0109 mL5.0543 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

You can also refer to dose conversion for different animals. More Dose Conversion

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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