Target nature :
Aurora kinases A/B
CAS n° :
133712-17-1
Mecanism of action :
Prevention of Histone 3 phosphorylation in mitotic cells
Physico-chemical properties :
Molecular weight: 292.33 g.mol-1
Probe availability :
Chimiothèque Institut Curie-CNRS
Princeps reference :
Cell Cycle 2009 8:5, 765 doi.org/10.4161/cc.8.5.7879 WO 2012 163934
More bibliography :
Other derivatives of the same family were reported active on Aurora kinases:Oncotarget, 2015, 22152 doi.org/10.18632/oncotarget.4158 Biology open 2013, 2:379 doi.org/10.1242/bio.20133079
Other available information on the probe :
Poor solubility. More soluble derivatives have been prepared (see Oncotarget).
Other information on the target :
NA
Selectivity profile :
36 different kinases profiling
In vivo data :
Some potency towards NSCLC agressive tumors.100 µg/20 g in PEG300/PBS/DMSO (5/4/1) was injected intraperitoneally in Swiss nude mice xenografted tumors (H358, Non Small Cancer Lung Cells) four times a week during two months.
In vitro data :
IC50 (Aurora kinase A)= 61 nM IC50 (Aurora kinase B)= 31 nM IC50 (Aurora kinase C)= 124 nM IC50 (H358, Non Small Cancer Lung Cells)= 145 nM IC50 (spheroid HCT-116)= 1.07µM
Toxicity :
Repetitive injections of C1 were well tolerated by the animals.
Chaine SMILES :
CCc1c[nH]c(=O)c4c1[nH]c3ccc2cc(OC)ccc2c34
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