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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)-BAY-1816032
BAY-1816032

Chemical Structure : BAY-1816032

CAS No.: 1891087-61-8

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BAY-1816032 (BAY1816032)

货号: 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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5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3580 In stock
50 mg ￥5680 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 534.524
分子式 C27H24F2N6O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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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