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Chemical Structure : BAY-1816032
CAS No.: 1891087-61-8
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
| 25 mg | $358 | In stock | |
| 50 mg | $568 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 534.524 | |
| Formula | C27H24F2N6O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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