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Background Information:
BAY-1816032 is an orally available, highly potent and selective BUB1 (Mitotic checkpoint serine/threonine-protein kinase) inhibitor, with an enzymatic IC50 of 7 nM, and highly selective against other 395 kinases. Mechanistically BAY 1816032 abrogated nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with an IC50 of 29 nM, induced lagging chromosomes and mitotic delay (ref 1). Demonstrated in vitro and in vivo antitumor efficacy when applied in combination with taxanes (ref 1).
Reference:
1. Gerhard Siemeister, et al, Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. Abstract 287: BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity* confirmed by a spot-on high precision quantitative elemental analysis.
APIM050020: BAY-1816032
CAS No.: 1891087-61-8.
Molecular Formula: C27H24F2N6O4.
Molecular Weight: 534.5 (or refer to Certificate of Analysis, batch specific).
Purity: 99.9% (HPLC at 214 and 254 nm).
QC: HPLC-MS, NMR and Quantitative Elemental Analysis.
Solubility: refer to certificate of analysis.
Storage: refer to certificate of analysis.
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