New potent, selective and non toxic c-kit inhibitors

Details New potent, selective and non toxic c-kit inhibitors New potent, selective and non toxic c-kit inhibitors

G - Physics

01

N

G01N 33/48 (2006.01) A61K 31/00 (2006.01) A61K 31/015 (2006.01) A61K 31/095 (2006.01) A61K 31/40 (2006.01) A61K 31/403 (2006.01) A61K 31/404 (2006.01) A61K 31/415 (2006.01) A61K 31/4709 (2006.01) A61K 31/498 (2006.01) A61K 31/505 (2006.01) A61K 31/506 (2006.01) A61K 31/517 (2006.01) A61K 31/519 (2006.01) A61K 45/06 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2452368

The present invention relates to a screening method allowing the identification and selection of compounds targeting the transphosphorylase (also called phosphotransferase) domain of c-kit, more particularly compounds selected to be potent inhibitors of constitutively activated c-kit, while being unable to inhibit other activation pathways such as for example the pathways leading to death of IL-3 dependent cells cultured in presence of IL-3.

La présente invention concerne une méthode de criblage permettant d'identifier et de sélectionner des composés visant le domaine transphosphorylase (également appelé phosphotransférase) de c-kit, plus particulièrement, des composés choisis pour être des inhibiteurs puissants de c-kit à activité constitutive, et pour inhiber d'autres voies d'activation, telles que, par exemple, les voies entraînant la mort des cellules dépendantes de IL-3 cultivées en présence de IL-3.

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