BAY 1816032

Pricing Availability   Qty
Description: Potent and selective BUB1 kinase inhibitor
Chemical Name: 2-[3,5-Difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]ethanol
Purity: ≥98% (HPLC)
Literature (2)

Biological Activity for BAY 1816032

BAY 1816032 is a potent and selective inhibitor of BUB1 kinase, a mitotic checkpoint serine/threonine kinase (IC50 = 6.1 nM). BAY 1816032 shows 17-fold selectivity over a panel of 403 other human kinases. In vivo, BAY 1816032 decreases tumor size in tumor xenograft models. BAY 181603 is orally bioavailable.

Compound Libraries for BAY 1816032

BAY 1816032 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for BAY 1816032

M. Wt 534.52
Formula C27H24F2N6O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1891087-61-8
PubChem ID 118958833

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BAY 1816032

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 26.73 50

Preparing Stock Solutions for BAY 1816032

The following data is based on the product molecular weight 534.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 3.74 mL 18.71 mL 37.42 mL
2.5 mM 0.75 mL 3.74 mL 7.48 mL
5 mM 0.37 mL 1.87 mL 3.74 mL
25 mM 0.07 mL 0.37 mL 0.75 mL

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References for BAY 1816032

References are publications that support the biological activity of the product.

Siemeister et al (2019) Inhibition of BUB1 kinase by BAY 1816032 sensitizes tumor cells toward taxanes, ATR, and PARP inhibitors in vitro and in vivo. Clin.Cancer Res. 25 1404 PMID: 30429199

If you know of a relevant reference for BAY 1816032, please let us know.

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Citations for BAY 1816032

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Literature in this Area

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Cell Cycle and DNA Damage Research Product Guide

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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.