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BAY-1816032

Catalog No. T10467 CAS 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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BAY-1816032, CAS 1891087-61-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
5 mg	In stock	$ 128.00
10 mg	In stock	$ 213.00
25 mg	In stock	$ 425.00
50 mg	In stock	$ 628.00
100 mg	In stock	$ 896.00
1 mL * 10 mM (in DMSO)	In stock	$ 153.00

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Purity: 99.32%

Purity: 98.92%

Purity: 98.02%

Biological Description

Chemical Properties

Storage & Solubility Information

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.

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 20 mg/mL (37.42 mM), Sonification and heating are recommended.

References and Literature

1. Siemeister G, et al. BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Ishington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 287. doi:10.1158/1538-7445.AM2017-287

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library NO PAINS Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

BAY-1816032 1891087-61-8 Others inhibit Inhibitor BAY 1816032 BAY1816032 inhibitor

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