Nutlin-3 - CAS:548472-68-0 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Nutlin-3
英文名称:	Nutlin-3
别名:	(±)-4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
CAS No:	548472-68-0	分子式:	C₃₀H₃₀Cl₂N₄O₄	分子量:	581.49
CAS No:	548472-68-0
分子式:	C₃₀H₃₀Cl₂N₄O₄
分子量:	581.49
MDL:	MFCD11977784

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N10039 Nutlin-3 ≥98% (HPLC) (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(20mg/ml)和乙醇。

产品描述：

基本信息

产品编号：N10039
产品名称：Nutlin-3
CAS:	548472-68-0	储存条件	粉末	-20℃	四年

分子式：	C30H30Cl2N4O4		溶于液体	-80℃	六个月
分子量	581.49			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	100mg/mL (171.96mM)
		Ethanol	100mg/mL (171.96mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.7197mL	8.5985mL	17.1969mL
5mM	0.3439mL	1.7197mL	3.4394mL
10mM	0.1720mL	0.8598mL	1.7197mL
50mM	0.0344mL	0.1720mL	0.3439mL

生物活性

产品描述	一种有效的 p53-MDM2 抑制剂，IC50：0.09μM。
靶点/IC50	Mdm2 (Cell-free assay)
靶点/IC50	180nM
体外研究	Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1μM of Inauhzin and 2μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3μM) but has minimal toxicity toward p53-deficient cells (IC50, >10μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines.
体内研究	Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo.

推荐实验方法(仅供参考)

激酶实验：

Biacore 研究

在Biacore S51上进行竞争性实验。衍生一系列S传感器芯片CM5，用于固定 PentaHis抗体，为了捕获 His-标记的p53。捕获的水平为~200反应单位(1 反应单位对应于1 pg 蛋白/ mm2)。MDM2蛋白浓度一直维持在300nM。Nutlin-3 溶于DMSO，浓度为10mM，然后进一步稀释，在每个MDM2实验样本中产生系列浓度的Nutlin-3。在电泳缓冲液(10mM Hepes,0.15M NaCl, 2% DMSO)中25oC下进行实验。在Nutlin-3存在时，计算MDM2-p53结合情况，作为结合百分数，使用Microsoft Excel计算IC50。

细胞实验:

Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates,and incubated at 37℃ overnight. After treatment of Inauhzin and Nutlin 3 at the indicated concentrations for 48h, cells are harvested,fixed in 70% ice-cold ethanol overnight at -20℃, resuspended in propidium iodide-solution (50µg/mL PI, 0.1mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37℃,then analyzed for DNA content using a flow cytometer and proprietary software.

动物实验:

Mice

Five-week-old female SCID mice are used. Mice are subcutaneously inoculated with 3×106 HCT116p53+/+ cells in the right flank and tumor growth is monitored with calipers. After the mean tumor volume reaches 50-100 mm3, animals are administered Inauhzin intraperitoneally (IP), Nutlin 3 orally, or vehicles (4% DMSO for Inauhzin, EtOH: Tween: 5% Glucose=5:5:90 for Nutlin 3). Tumor volume is measured every other day, and inhibition of tumor growth (T/C) is calculated on the last day of treatment.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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