MD-224 是基于蛋白水解定位嵌合体 (PROTAC) 的高效小分子 (MDM2) 降解物。MD-224 在人白血病细胞中，诱导 MDM2 的快速降解 (<1 nm)，抑制 rs4;11 细胞生长的 ic50 值为 1.5 nm。md-224 有可能成为一类新的抗癌剂。
货号:ajcx15408
CAS:2136247-12-4
分子式:C48H43Cl2FN6O6
分子量：889.8
溶解度:DMSO: 150 mg/mL (168.58 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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