BAY 1816032

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Cat.No. 7549 - BAY 1816032 | C27H24F2N6O4 | CAS No. 1891087-61-8
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)
Datasheet
Citations
Reviews
Literature (4)

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.

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.

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


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Citations for BAY 1816032

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