BI-0252 |
رقم الكتالوجGC35511 |
BI-0252 هو مثبط انتقائي MDM2-p53 نشط عن طريق الفم مع IC50 من 4 نانومتريمكن أن يؤدي BI-0252 إلى حدوث تراجع في الورم في جميع حيوانات الفأر SJSA-1 xenograft ، مع ما يصاحب ذلك من تحريض جينات مستهدفة لبروتين الورم p53 (TP53) وعلامات موت الخلايا المبرمج
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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.
Average Rating: 5
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