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BAY-1816032

Name: BAY-1816032
Brand: TargetMol
SKU: T10467
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10467Cas No. 1891087-61-8

BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.

BAY-1816032

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Purity: 99.81%

Catalog No. T10467Cas No. 1891087-61-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$32	In Stock	In Stock
5 mg	$77	In Stock	In Stock
10 mg	$128	In Stock	In Stock
25 mg	$255	In Stock	In Stock
50 mg	$377	In Stock	In Stock
100 mg	$538	In Stock	In Stock
200 mg	$738	-	In Stock
1 mL x 10 mM (in DMSO)	$92	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:99.81%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.
Targets&IC50	BUB1 kinase:7 nM
In vitro	METHODS: BAY-1816032 (0, 1.5625, 3.125, 6.25, 12.5, 25, 50 μM, 48 hours) treated ATC cells (TPC-1, 8505C), and CCK-8 assay was used to study cell viability. RESULTS BAY-1816032 treatment resulted in a decrease in ATC cell viability, with IC50 values of 4.230 μM in TPC-1 cells and 6.216 μM in 8505C cells. [2] METHODS: Colony formation assay, cell cycle, invasion, migration and wound healing assay were performed after ATC cells were treated with BAY-1816032 (0, 2.5, 5 μM). RESULTS BAY-1816032 can significantly reduce colony formation ability; BAY-1816032 can cause cell cycle arrest similar to siRNA; BAY-1816032 treatment can significantly hinder the invasion and migration of ATC cells in a dose-dependent manner. [2]
In vivo	METHODS: BAY-1816032 (100 mg/kg, oral, 24 days) was used to treat 8505C xenograft model mice to evaluate the anti-ATC activity and safety of BAY-1816032 in mice. RESULTS There was no significant difference in the body weight of each group of mice; the tumor weight of mice treated with BAY-1816032 was significantly reduced. [2]

Chemical Properties

Molecular Weight	534.51
Formula	C₂₇H₂₄F₂N₆O₄
Cas No.	1891087-61-8
Smiles	COc1cnccc1Nc1nc(ncc1OC)-c1nn(Cc2c(F)cc(OCCO)cc2F)c2ccccc12
Relative Density.	1.40 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

H2O: < 0.1 mg/mL (insoluble)

DMSO: 25 mg/mL (46.77 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.74 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	1.8709 mL	9.3544 mL	18.7087 mL	93.5436 mL
5 mM	0.3742 mL	1.8709 mL	3.7417 mL	18.7087 mL
10 mM	0.1871 mL	0.9354 mL	1.8709 mL	9.3544 mL
20 mM	0.0935 mL	0.4677 mL	0.9354 mL	4.6772 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