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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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Biological Activity

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; abrogates nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with IC50 of 29 nM, induces lagging chromosomes and mitotic delay, inhibits proliferation of various tumor cell lines with mean IC50 of 1.4 uM; demonstrates synergy or additivity with paclitaxel or docetaxel both in vitro and in vivo.

Physicochemical Properties

M.Wt 534.524
Formula C27H24F2N6O4
CAS No. 1891087-61-8
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

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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