General information
CAS n°
133712-17-1
Mechanism 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