计算溶液所需的质量、体积或浓度。
概述
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 consists of ligands for Cereblon and MDM2 . MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC 50 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
In Vitro
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. 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. MD-224 (0.001-1 μM; 24 hours) induces robust apoptosis at ≤10 nM in a dose-dependent manner upon a 24 hours treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: RS4;11 cells Concentration: 1 nM; 3 nM; 10 nM; 30 nM Incubation Time: 2 hours Result: Decreased MDM2 protein and accumulated of p53 protein. RT-PCRCell Line: RS4;11 cells Concentration: 30 nM Incubation Time: 6 hours Result: Upregulated p53 target gene expression. Apoptosis AnalysisCell Line: RS4;11 cells Concentration: 0.001 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM Incubation Time: 24 hours Result: Induces robust apoptosis in RS4;11 cells.
IC50& Target:MDM2 1 nM (IC 50 )
规格
规格或纯度
10mM in DMSO
英文名称
MD-224
生化机理
MD-224是一种基于蛋白酶靶向嵌合体（PROTAC）概念的首创高效小分子人鼠双分化2（MDM2）降解剂。MD-224 由脑龙和 MDM2 的配体组成。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CCC2(CC1)[C@@]3([C@H]([C@@H](N2)C(=O)NC4=CC=C(C=C4)C(=O)NCCCC#CC5=C6CN(C(=O)C6=CC=C5)C7CCC(=O)NC7=O)C8=C(C(=CC=C8)Cl)F)C9=C(C=C(C=C9)Cl)NC3=O
PubChem CID
分子量
889.80
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 SSE:688179 保留所有权利。
危险品化学品经营许可证（带存储）