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BI-847325

Name: BI-847325
Brand: TargetMol
SKU: T6785
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6785Cas No. 1207293-36-4

BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.

BI-847325

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Purity: 97.54%

Catalog No. T6785Cas No. 1207293-36-4

BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
5 mg	$93	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$446	In Stock	In Stock
100 mg	$662	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$96	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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Purity:97.54%

Color:White

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COA

Product Introduction

Bioactivity

Description	BI-847325 is a selective dual inhibitor of MEK and aurora kinases (AK) with IC50 values of 4 and 15 nM for human MEK2 and AK-C, respectively.
Targets&IC50	Aurora kinase:15 nM, MEK:4nM
In vitro	BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression. [1]
In vivo	In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights. [1]
Kinase Assay	Assays are run in the presence of 100 μM ATP using 10 μM of substrate. 30 μL PROTEIN-MIX in 25% DMSO and incubated for 15 min at room temperature. 10 μL PEPTIDE-MIX is added, the mixture is incubated for 60 min at RT and stopped by adding 180 μL 6.4% TCA (final concentration: 5%). Incorporated phosphate is measured in a scintillation counter and IC50 values are calculated using a sigmoidal curve analysis program with variable hill slope[1].
Cell Research	Cells are plated at a density of 2.5 × 103 cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturer's protocol.(Only for Reference)

Chemical Properties

Molecular Weight	464.56
Formula	C₂₉H₂₈N₄O₂
Cas No.	1207293-36-4
Smiles	CCNC(=O)C#Cc1ccc2\C(=C(\Nc3ccc(CN(C)C)cc3)c3ccccc3)C(=O)Nc2c1
Relative Density.	no data available

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: 18 mg/mL (38.75 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 1 mg/mL (2.15 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.15 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

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1526 mL	10.7629 mL	21.5257 mL	107.6287 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.4305 mL	2.1526 mL	4.3051 mL	21.5257 mL
10 mM	0.2153 mL	1.0763 mL	2.1526 mL	10.7629 mL
20 mM	0.1076 mL	0.5381 mL	1.0763 mL	5.3814 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