MMRi62

CAS: 352693-80-2 货号: M648525 分子式: C21H15Cl2N3O 分子量: 396.27
有货
级别和纯度: ≥99%
储存条件
避光,-80℃储存
运输条件
特低温运输
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规格
库存
价格
数量
5mg
M648525-5mg
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¥850.90
10mg
M648525-10mg
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¥1,450.90
25mg
M648525-25mg
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¥3,000.90
50mg
M648525-50mg
期货 Stock Image
¥4,850.90
100mg
M648525-100mg
期货 Stock Image
¥7,800.90
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为什么选择此级别

提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

避光,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 induces ferroptosis , resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12.

In Vitro

MMRi62 inhibits proliferation, clonogenic, and spheroid growth of pancreatic ductal adenocarcinoma cell (PDAC) by induction of cell death. 1\nMMRi62 (3 nM-100 μM;4 h) binds to RING–RINGheterodimers of MDM2 and MDM4 withthe K d value of 1.39 μM. MMRi62 (10 nM-1 μM;72 h) induces apoptosis and inhibits leukemic cells with IC 50 sof 0.34 µM (HL60) and 0.22 µM (HL60VR). MMRi62 (5 μM and 10μM; 24 h) decreases MDM2B autoubiquitination, increasesMDM4 ubiquitination in a dose-dependent manner. MMRi62 is an E3 ligase modifier capable ofswitching substrate preference from MDM2 to MDM4. MMRi62 (5 μM; 24and 72 h) induces apoptosis in a p53-independent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: WT-p53 bearing MV4-11 cells; 293cells transfected with MDM2B and MDM4 Concentration: 2, 2.5, 5, 10, 40, 80, 160 μM Incubation Time: 24 hours Result: Increased cleaved PARP protein and activatedcaspase 3 level in wt-p53 bearing MV4-11 cells at 2 μM for 24 h. Decreased MDM2B autoubiquitination, increasedMDM4 ubiquitination at 5 μM and 10 μM for 24 h. Induced MDM2-dependent degradation of MDM4protein at 5 μM in NALM6 cells. Cell Proliferation AssayCell Line: Primary AML patient cells, NALM6cells and NALM6shp53 cells Concentration: 1, 10, 25, and 50 µM Incubation Time: 24 hours and 72 hours Result: Induced NALM6 cells apoptosis at 24 hand induced Primary AML patient cells at 72 h.

In Vivo

MMRi62 shows anti-tumor activity in orthotopic xenograft PDAC mouse models, by inhibiting tumor growth in mice associated with downregulation of NCOA4 and mutant p53 . MMRi62 also completely abrogates metastasis of orthotopic tumors . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

规格

规格或纯度
≥99%
英文名称
MMRi62
生化机理
MMRi62 是一种针对 MDM2-MDM4(肿瘤抑制因子 p53 的负调控因子)的铁凋亡诱导剂。MMRi62 对胰腺导管腺癌(PDAC)细胞具有不依赖于 P53 的促凋亡活性,并能诱导自噬。 MMRi62 诱导铁变态反应
储存条件
避光,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
396.27

技术文档

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高级数据

化学和物理性质
溶解性
DMSO : 62.5 mg/mL (157.72 mM; ultrasonic and warming and heat to 60°C)
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