Target nature :
Tubuline colchicine site
CAS n° :
2324119-74-4
Mecanism of action :
Microtubule destabilizing agent
Physico-chemical properties :
Molecular weight: 400.47 g.mol-1 90mM in DMSO at 25°C
Probe availability :
Chimiothèque Institut Curie-CNRS (UMR9187-U1196)
Princeps reference :
Gilson, P.; Josa-Prado, F.; Beauvineau, C.; Naud-Martin, D.; Vanwonterghem, L.; Mahuteau-Betzer, F.; Moreno, A.; Falson, P.; Lafanechère, L.; Frachet, V.; Coll, J-L; Fernando Díaz, J.; Hurbin, A.; Busser B. Identification of pyrrolopyrimidine derivative PP-13 as a novel microtubule-destabilizing agent with promising anticancer properties. Scientific Reports 2017:10209.
More bibliography :
Gilson, P.; Couvet, M.; Vanwonterghem, L.; Henry, M.; Vollaire, J.; Baulin, V.; Werner, M.; Orlowska, A.; Josserand, V.; Mahuteau-Betzer, F.; Lafanechère, L.; Coll, J.-L.; Busser, B.; Hurbin, A. The pyrrolopyrimidine colchicine-binding site agent PP-13 reduces the metastatic dissemination of invasive cancer cells in vitro and in vivo. Biochemical Pharmacology 2019, 160, 1-13
Other available information on the probe :
no other information
Other information on the target :
no other information available
Selectivity profile :
Kinome array (460 kinases-Discoverx) at 10 µM : no kinase inhibition
In vivo data :
Low concentration PP-13 (130 nmol.L¿1) treatment significantly reduced the metastatic invasiveness of human cancer cells engrafts on chicken chorioallantoic membrane. In nude mice, 0.5 or 1 mg.kg¿1 PP-13 intraperitoneally administered three-times a week reduced the sizes of paclitaxel-refractory orthotopic breast tumors, delayed the progression of metastasis, and decreased the global metastatic load compared to 0.5 mg.kg¿1 paclitaxel or vehicle alone.
In vitro data :
PP-13 induced a mitotic blockade and apoptosis in several cancer cells cultured in two-dimensions or three-dimensions spheroids, in conjunction with reduced cell proliferation. It also inhibited cancer cell motility and invasion, in in vitro wound-healing and transwell migration assays.
Toxicity :
PP-13 did not show any apparent early adverse effect in vivo.
Chaine SMILES :
CCOC(=O)c4ccc(Cn3c(C)cc2c(NCc1ccccc1)ncnc23)cc4
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