CAY10682 - CAS:1542066-74-9

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CAY10682 (Synonyms:p53-MDM2-IN-3)

目录号 : KCM11637 CAS No. : 1542066-74-9 纯度 : ≥98%

Data Sheet 产品使用指南

(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (K = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKKɛ (ICs = 80.5, 78.2, and 57.1 µM, respectively). CAY10682 blocks the growth of cancer cells in vitro (ICs = 2-6 µM) and inhibits the growth of A549 cell xenografts in mice without significantly reducing body weight.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

CAY10682 is an orally active p53-MDM2 inhibitor with a Ki value of 0.25 μM. CAY10682 exerts antitumor activity by inhibiting NF-κB pathway.

体外研究

CAY10682 (0.1-20 μM, 4 h) dose dependently increased p65 levels in the cytoplasm and nucleus of A549 cells.
CAY10682 (0.1-10 μM, 4 h) selectively activates p53 or inhibits the NF - κ B pathway in A549 cells.

Western Blot Analysis

Cell Line:	A549
Concentration:	0.1, 1, 10 μM
Incubation Time:	4 hour
Result:	Activated the phosphorylation of IKKβ only or both IKKβ and IKKα in a dose-dependent manner.

体内研究

CAY10682 (200 mg/kg, gavage, 14 days) effectively inhibited tumor growth in A549 xenograft model.

分子式

C₃₀H₂₅BrFN₅O

分子量

570.45

CAS号

1542066-74-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： ≥98%

Data Sheet

产品使用指南

Zhuang C, et al. Double-edged swords as cancer therapeutics: novel, orally active, small molecules simultaneously inhibit p53-MDM2 interaction and the NF-κB pathway. J Med Chem. 2014 Feb 13;57(3):567-77.

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The dilution calculator equation

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体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

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2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

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动物实验计算换算器