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ET-D5

Target nature : Protein Phosphatase 1
CAS n° : 181371-85-7
Mecanism of action : Microtubule destabilizing agent
Physico-chemical properties : Molecular weight 326.30 g.mol-1 Soluble in water 0.2 mg/mL Soluble in aqueous solution (8 mg/ml) of beta-cyclodextrine (60 mg/ ml)
Probe availability : Chimiothèque Institut Curie-CNRS
Princeps reference : WO 2011 107709
More bibliography : Tetrahedron 1996, 52, 10427 doi.org/10.1016/0040-4020(96)00579-0
Other available information on the probe : NA
Other information on the target : NA
Selectivity profile : NA
In vivo data : 200 mg/kg per os twice a week during two months led to necrosis of xenografted tumor (NCI-460 HTB177). ET-D5 in aqueous solution (8 mg/ml) of beta-cyclodextrine (60 mg/ ml)
In vitro data : IC50≤ 9 μΜ on PPICA (Subcatalytic unit of PP1, alpha isoform) GI50<0.1 µM on HMEC cells
Toxicity : Cellular toxicity: IC50 (fibroblast) = 6µM >> IC50 (HUVEC) = 60nM
Chaine SMILES : COc3ccc(c2[nH]c(=O)c1cc(OC)ccc1c2N(=O)=O)cc3
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