APL-5125 (APL5125)

Chemical Structure : APL-5125

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货号: PC-25618Not For Human Use, Lab Use Only.

APL-5125 is a highly potent, selective, ATP-competitive casein kinase 2α (CK2α) inhibitor with IC50 of 0.348 nM and Ki of 0.095 nM in ADP-GloTM Assays, >300-fold selective over CLK2 and DAPK3.

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生物&药学活性

APL-5125 is a highly potent, selective, ATP-competitive casein kinase 2α (CK2α) inhibitor with IC50 of 0.348 nM and Ki of 0.095 nM in ADP-GloTM Assays, >300-fold selective over CLK2 and DAPK3.
APL-5125 shows bivalent binding mode extending to the cryptic αD pocket of CK2α.
APL-5125 has >175-fold selectivity over the nearest kinases DAPK1 and DAPK3, also shows clear selectivity against a panel of 87 enzymes, ion channels, receptors and transporters.
APL-5125 shows very potent cellular inhibition of CK2α that is >150-fold more potent than silmitasertib.
APL-5125 potently inhibits p-AKT S129 (IC50 =2 nM) in vitro in human peripheral blood mononuclear cells (PBMCs).
APL-5125 (10, 30, 100 mg/kg) inhibits p-AKT S129 in HCT116-tumors in mice following oral administration.

物理化学性质&存储条件

分子量	565.50
分子式	C27H24F5N3O5
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	5-(2-(4-((3,5-Difluoro-4-(trifluoromethoxy)benzyl)amino)butoxy)ethoxy)benzo[c][2,6]naphthyridine-8-carboxylic acid

参考文献

1. Glossop PA, et al. J Med Chem. 2025 Oct 14. doi: 10.1021/acs.jmedchem.5c01807.

APL-5125 (APL5125)

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物理化学性质&存储条件

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APL-5125 (APL5125)

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物理化学性质&存储条件

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