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Submit ReviewBAY 1816032
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)
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 |
| InChI Key | QVOGVAVHOLLLAZ-UHFFFAOYSA-N |
| Smiles | COC1=CN=C(N=C1NC2=C(C=NC=C2)OC)C3=NN(C4=CC=CC=C43)CC5=C(C=C(C=C5F)OCCO)F |
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for BAY 1816032
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
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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
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
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Cell Cycle & DNA Damage Repair Poster
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.