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BO-264

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Catalog No. T8492Cas No. 2408648-20-2

BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with an IC50 of 188 nM and a Kd of 1.5 nM.

BO-264

BO-264

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Purity: 99.81%
Catalog No. T8492Cas No. 2408648-20-2
BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with an IC50 of 188 nM and a Kd of 1.5 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$32In StockIn Stock
5 mg$73In StockIn Stock
10 mg$123In StockIn Stock
25 mg$197In StockIn Stock
50 mg$297In StockIn Stock
100 mg$446-In Stock
1 mL x 10 mM (in DMSO)$80In 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:99.81%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with an IC50 of 188 nM and a Kd of 1.5 nM.
Targets&IC50
TACC3:188 nM (IC50), TACC3:1.5 nM (Kd)
In vitro
BO-264 demonstrated superior antiproliferative activity to the two currently reported TACC3 inhibitors, especially in aggressive breast cancer subtypes, basal and HER2+, via spindle assembly checkpoint-dependent mitotic arrest, DNA damage, and apoptosis, while the cytotoxicity against normal breast cells was negligible.?Furthermore, BO-264 significantly decreased centrosomal TACC3 during both mitosis and interphase.?BO-264 displayed potent antiproliferative activity ( 90% have less than 1 μmol/L GI50 value) in the NCI-60 cell line panel compromising of nine different cancer types.?Noteworthy, BO-264 significantly inhibited the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies.?Importantly, its oral administration significantly impaired tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increased survival without any major toxicity.?Finally, TACC3 expression has been identified as strong independent prognostic factor in breast cancer and strongly prognostic in several different cancers.
Chemical Properties
Molecular Weight353.38
FormulaC18H19N5O3
Cas No.2408648-20-2
SmilesCOc1ccc(cc1)-c1cc(Nc2ccnc(n2)N2CCOCC2)on1
Relative Density.1.306 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: 50 mg/mL (141.49 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.66 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 mM2.8298 mL14.1491 mL28.2981 mL141.4907 mL
5 mM0.5660 mL2.8298 mL5.6596 mL28.2981 mL
10 mM0.2830 mL1.4149 mL2.8298 mL14.1491 mL
20 mM0.1415 mL0.7075 mL1.4149 mL7.0745 mL
50 mM0.0566 mL0.2830 mL0.5660 mL2.8298 mL
100 mM0.0283 mL0.1415 mL0.2830 mL1.4149 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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