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Borussertib

Name: Borussertib
Brand: TargetMol
SKU: T8427
Price: 135 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8427Cas No. 1800070-77-2

Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.

Borussertib

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Purity: 99.00%

Catalog No. T8427Cas No. 1800070-77-2

Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$135	In Stock	In Stock
5 mg	$289	In Stock	In Stock
10 mg	$455	In Stock	In Stock
25 mg	$753	-	In Stock
50 mg	$1,060	-	In Stock
100 mg	$1,430	-	In Stock
1 mL x 10 mM (in DMSO)	$379	In Stock	In 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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Batch Information

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Purity:99.00%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR HPLC

Product Introduction

Bioactivity

Description	Borussertib is a first-in-class covalent-allosteric inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.
Targets&IC50	Akt (WT):0.8 nM, Akt (WT):2.2 nM （ki）
In vitro	Borussertib exhibits excellent cellular activity in the nanomolar range with superior profile against clinical candidate Akt inhibitors as well as the cytostatic drug doxorubicin. With the EC50 values are 191±90 nM, 48±15 nM, 5±1 nM, 277±90 nM, 373±54 nM, 7770±641 nM in AN3CA (endometrium), T47D (breast), ZR-75-1 (breast), MCF-7 (breast), BT-474 (breast) and KU-19-19 (bladder) cell lines, respectively[1].

Chemical Properties

Molecular Weight	596.68
Formula	C₃₆H₃₂N₆O₃
Cas No.	1800070-77-2
Smiles	C=CC(=O)Nc1ccc2[nH]c(=O)n(C3CCN(Cc4ccc(cc4)-c4nc5cc[nH]c(=O)c5cc4-c4ccccc4)CC3)c2c1
Relative Density.	1.318 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 25 mg/mL (41.9 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.35 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

	1mg	5mg	10mg	50mg
1 mM	1.6759 mL	8.3797 mL	16.7594 mL	83.7970 mL
5 mM	0.3352 mL	1.6759 mL	3.3519 mL	16.7594 mL
10 mM	0.1676 mL	0.8380 mL	1.6759 mL	8.3797 mL
20 mM	0.0838 mL	0.4190 mL	0.8380 mL	4.1899 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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