PLK1 inhibitor B9

Chemical Structure : PLK1 inhibitor B9

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货号: PC-27199Not For Human Use, Lab Use Only.

PLK1 inhibitor B9 is a potent, selective, covalent inhibitor of polo-like kinase 1 (PLK1) with IC50 of 19 nM, shows exceptional cellular potency with IC50 of 0.4 nM in K562 leukemia cells.

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200 mg		Get quote

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生物&药学活性

PLK1 inhibitor B9 is a potent, selective, covalent inhibitor of polo-like kinase 1 (PLK1) with IC50 of 19 nM, shows exceptional cellular potency with IC50 of 0.4 nM in K562 leukemia cells.
B9 shows >150-fold improvement over the reversible reference compound BI2536 (K562 cell IC50=61 nM).
K562 shows favorable overall selectivity against nonrelated kinases.
B9 (10-20 mg/kg, i.p.) significantly suppressed the bioluminescence of leukemia burden and extended survival rates to 100% over 42 days without observable toxicity.

物理化学性质&存储条件

分子量	551.62
分子式	C28H34FN7O4
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	(R)-4-((8-(1-acryloylpiperidin-4-yl)-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl)amino)-N-cyclopropyl-2-fluoro-5-methoxybenzamide

参考文献

1. Zhou J, et al. J Med Chem. 2026 Jun 30. doi: 10.1021/acs.jmedchem.6c01512.