BAY-1816032|BAY1816032|CAS 1891087-61-8

Cas No.:	1891087-61-8
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
Synonyms:	BAY1816032
SMILES:	COC1=C(NC2=NC(C3=NN(CC4=C(F)C=C(OCCO)C=C4F)C5=C3C=CC=C5)=NC=C2OC)C=CN=C1
Formula:	C₂₇H₂₄F₂N₆O₄
M.Wt:	534.524
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Siemeister G, et al. BAY 1816032, a novel BUB1 kinase inhibitor with potent antitumor activity [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Ishington, DC. Philadelphia (PA): AACR; Canc

Description:

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.

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