您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > MN58b
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MN58b
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MN58b图片
CAS NO:203192-01-2
包装:1mg
市场价:2450元

产品介绍
MN58b 是一种选择性的 choline kinase α (CHKα) 抑制剂,可抑制磷酸胆碱的合成。MN58b 通过诱导凋亡来减少细胞生长,并具有抗肿瘤活性。
Cas No.203192-01-2
Canonical SMILESCN(C)C1=CC=[N+](C=C1)CC2=CC=C(CCCCC3=CC=C(C[N+]4=CC=C(N(C)C)C=C4)C=C3)C=C2.[Br-].[Br-]
分子式C32H40Br2N4
分子量640.49
溶解度DMSO: 14.71 mg/mL (22.97 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity[1][2].

The IC50s of MN58b for parental and Gemcitabine-resistant Suit2 007 cells are 3.14 µM and 0.77 µM, respectively[1].MN58b (1-5 µM; 72 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) has a marked effect on colony formation at 1 µM, and growth is completely abolished at 5 µM in all the cell lines[1].MN58b ((1-10 µM; 24-48 hours; SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells) induces apoptosis and this response correlates with CHKα expression[1]. Cell Viability Assay[1] Cell Line: SK-PC-1, Suit2 008, IMIM-PC2, and RWP-1 cells

MN58b (4 mg/kg; intraperitoneal injection; once a day; for 5 days; MF-1 nude mice) treatment significantly decreases phosphomonoesters in both HT29 and MDA-MB-231 xenografts. Phosphocholine levels are found to correlate with choline kinase activities[2]. Animal Model: MF-1 nude mice with HT29 or MDA-MB-231 cells[2]

[1]. Mazarico JM, et al. Choline Kinase Alpha (CHKα) as a Therapeutic Target in Pancreatic Ductal Adenocarcinoma: Expression, Predictive Value, and Sensitivity to Inhibitors. Mol Cancer Ther. 2016 Feb;15(2):323-33. [2]. Al-Saffar NM, et al. Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models. Cancer Res. 2006 Jan 1;66(1):427-34.