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BAY-1816032

Chemical Structure : BAY-1816032

CAS No.: 1891087-61-8

BAY-1816032 (BAY1816032)

Catalog No.: PC-63128Not For Human Use, Lab Use Only.

BAY-1816032 (BAY1816032) is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BAY-1816032 (BAY1816032) is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM.
BAY-1816032 displays excellent selectivity on a panel of 395 kinases.
BAY-1816032 abrogates nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with IC50 of 29 nM.
BAY-1816032 induces lagging chromosomes and mitotic delay, inhibits proliferation of various tumor cell lines with mean IC50 of 1.4 uM.
BAY-1816032 demonstrates synergy or additivity with paclitaxel or docetaxel both in vitro and in vivo.

Physicochemical Properties

M.Wt 534.524
Formula C27H24F2N6O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-[3,5-Difluoro-4-[[3-[5-methoxy-4-[(3-methoxy-4-pyridinyl)amino]-2-pyrimidinyl]-1H-indazol-1-yl]methyl]phenoxy]ethanol

References

1. Gerhard Siemeister, et al. Abstract 287: BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity. AACR. DOI: 10.1158/1538-7445.

2. Siemeister G, et al. Clin Cancer Res. 2018 Nov 14. pii: clincanres.0628.2018.

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