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C1

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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