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BI-1347

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Catalog No. T5405Cas No. 2163056-91-3

BI-1347 is a potent, selective inhibitor of CDK8/cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.

BI-1347

BI-1347

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Purity: 99.63%
Catalog No. T5405Cas No. 2163056-91-3
BI-1347 is a potent, selective inhibitor of CDK8/cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$34In StockIn Stock
5 mg$80In StockIn Stock
10 mg$128In StockIn Stock
25 mg$253In StockIn Stock
50 mg$463In StockIn Stock
100 mg$682In StockIn Stock
500 mg$1,430-In Stock
1 mL x 10 mM (in DMSO)$89In 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:99.63%
Appearance:Solid
Color:White to Yellow
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Product Introduction

BI-1347 AI Summary
BI-1347 shows a broad spectrum of bioactivities, including inhibition of tau aggregation induced by a specific mutant tau, and inhibition of CDK8/CyclinC with a low IC50 value, demonstrating high binding affinity to CDK8. These features suggest potential therapeutic applications in neurodegenerative diseases and cancer. Moreover, this compound exhibits inhibitory activity against the SARS-CoV-2 3CL-Pro protease, with an inhibition percentage of -21.58% at a concentration of 20µM in a FRET assay and hinders SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10µM. It also influences cell viability in a cell-type-specific manner, demonstrating both positive and negative effects on the growth rates of HEK293T, U2OS, and human fibroblast cells. Additionally, the compound affects the thermal stability of various protein domains, increasing or decreasing their stability selectively. These diverse bioactivities underline the compound's potential as a multi-target therapeutic agent..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
BI-1347 is a potent, selective inhibitor of CDK8/cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.
Targets&IC50
CDK8:1 nM (cell free)
Chemical Properties
Molecular Weight356.42
FormulaC22H20N4O
Cas No.2163056-91-3
SmilesCN(C)C(=O)Cn1cc(cn1)-c1ccc(cc1)-c1cncc2ccccc12
Relative Density.no data available
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 120 mg/mL (336.68 mM), Sonication and heating are recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.22 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 mM2.8057 mL14.0284 mL28.0568 mL140.2839 mL
5 mM0.5611 mL2.8057 mL5.6114 mL28.0568 mL
10 mM0.2806 mL1.4028 mL2.8057 mL14.0284 mL
20 mM0.1403 mL0.7014 mL1.4028 mL7.0142 mL
50 mM0.0561 mL0.2806 mL0.5611 mL2.8057 mL
100 mM0.0281 mL0.1403 mL0.2806 mL1.4028 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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