MD-224 |
| Catalog No.GC38812 |
Le MD-224 est un dégradeur double minute 2 (MDM2) murin humain À petite molécule, premier de sa catégorie et très puissant, basé sur le concept de la chimère de ciblage de la protéolyse (PROTAC). MD-224 se compose de ligands pour Cereblon et MDM2. Le MD-224 induit une dégradation rapide de MDM2 À des concentrations <1 nM dans les cellules leucémiques humaines et atteint une valeur IC50 de 1,5 nM dans l'inhibition de la croissance des cellules RS4;11. Le MD-224 a le potentiel d'être une nouvelle classe d'agents anticancéreux.
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Cas No.: 2136247-12-4
Sample solution is provided at 25 µL, 10mM.
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MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1].
MD-224 (1-30 nM; 2 hours) effectively induces depletion of MDM2 protein and concurrently accumulation of p53 protein in a dose-dependent manner in RS4;11 cells[1].MD-224 (30 nM; 6 hours) is more potent than MI-1061 in induction of transcriptional upregulation of these p53 target genes but have no effect on TP53 itself in RS4;11 cells[1].MD-224 (0.001-1 μM; 24 hours) induces robust apoptosis at ≤10 nM in a dose-dependent manner upon a 24 hours treatment[1]. Western Blot Analysis[1] Cell Line: RS4;11 cells
[1]. Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis TargetingChimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable TumorRegression. J Med Chem. 2019 Jan 24;62(2):448-466
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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