BI-0252 |
Catalog No.GC35511 |
Le BI-0252 est un inhibiteur sélectif de MDM2-p53 actif par voie orale avec une IC50 de 4 nM. Le BI-0252 peut induire des régressions tumorales chez tous les animaux d'une xénogreffe SJSA-1 de souris, avec induction concomitante des gènes cibles de la protéine tumorale p53 (TP53) et des marqueurs d'apoptose.
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Cas No.: 1818291-27-8
Sample solution is provided at 25 µL, 10mM.
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis[1]. IC50: 4 nM (MDM2-p53)[1]
[1]. Gollner A, et al. Discovery of Novel Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction. J Med Chem. 2016 Nov 23;59(22):10147-10162.
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