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BAY-1816032

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Purity:99.32%

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COA HPLC HNMR

BAY-1816032

Catalog No. T10467Cas No. 1891087-61-8

BAY-1816032 is a potent and orally available inhibitor of bidding uninhibited by benzimidazoles 1 ( BUB1) kinase (IC50: 7 nM).

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Pack Size	Price	Availability
1 mg	$54	In Stock
5 mg	$128	In Stock
10 mg	$213	In Stock
25 mg	$425	In Stock
50 mg	$628	In Stock
100 mg	$896	In Stock
1 mL x 10 mM (in DMSO)	$153	In Stock

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Product Introduction

Bioactivity

Description	BAY-1816032 is a potent and orally available inhibitor of bidding uninhibited by benzimidazoles 1 ( BUB1) kinase (IC50: 7 nM).
Targets&IC50	BUB1 kinase:7 nM
In vitro	Mechanistically BAY-1816032 abrogates nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells (IC50: 29 nM), induced lagging chromosomes, and mitotic delay. Persistent lagging chromosomes and missegregation are observed in combination with low concentrations of paclitaxel. Single-agent BAY-1816032 inhibits the proliferation of various tumor cell lines with a median IC50 of 1.4 μM and demonstrates synergy or additivity with paclitaxel or docetaxel in almost all cell lines evaluated.
In vivo	In tumor xenograft studies, BAY 1816032 marginally inhibits tumor growth when administered orally as a single agent. However, when combined with paclitaxel or docetaxel, it significantly and notably reduces tumor size compared to the respective monotherapy treatments.

Chemical Properties

Molecular Weight	534.51
Formula	C27H24F2N6O4
Cas No.	1891087-61-8

Storage & Solubility Information

Storage

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

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 15 mg/mL (28.06 mM), Sonication and heating are recommended.

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 mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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

inhibitInhibitorBAY 1816032BAY1816032BAY-1816032