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NSC 146109 hydrochloride
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。
NSC 146109 hydrochloride图片
CAS NO:59474-01-0
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
NSC 146109 hydrochloride 是一种针对 MDMX 的小分子 p53 激活剂，可用于乳腺癌研究。 NSC 146109 hydrochloride 是一种假脲衍生物，通过激活 p53 和诱导促凋亡基因的表达来促进乳腺癌细胞凋亡。
Cas No.59474-01-0
化学名(10-methylanthracen-9-yl)methyl carbamimidothioate;hydrochloride
Canonical SMILESCC1=C2C=CC=CC2=C(C3=CC=CC=C13)CSC(=N)N.Cl
分子式C17H16N2S.HCl
分子量316.85
溶解度DMSO: 30 mg/ml,Ethanol: 3 mg/ml
储存条件Desiccate at RT
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

NSC 146109 hydrochloride is a selective activator of p53 with IC50 value ranges from 2.5 to >5 μg/mL [1].

Tumor protein p53 (p53) is a crucial protein in multicellular organisms and plays a pivotal role in preventing cancer formation. [1].

NSC 146109 hydrochloride is a potent p53 activator and has a higher activity than reported p53 activator RITA. When tested with breast tumor cell line MCF-7 cells, NSC 146109 hydrochloride treatment induced cell apoptosis and decreased cell viability through activating p53 expression which in turn up-regulated the expression of p21 [2]. In 16 tumor cells, NSC 146109 hydrochloride showed no clear genetic basis for the tumorigenic cell selectivity while had different affinity to different cell lines [1]. When tested with head and neck cancer (HNC) cell lines (high-expression of MDM4 while low-expression of p53, NSC 146109 hydrochloride treatment significantly suppressed cell growth and promoted cell apoptosis in a dose-dependent manner [3].

In mice model with head and neck cancer (HNC) cells subcutaneous xenograft, administration of NSC 146109 hydrochloride markedly inhibited cell growth and decreased tumor volume alone or combined with chemotherapy drug cisplatin which was regarded as a promising strategy for treating HNC in clinic [3].

References:
[1].  Dolma, S., et al., Identification of genotype-selective antitumor agents using synthetic lethal chemical screening in engineered human tumor cells. Cancer Cell, 2003. 3(3): p. 285-96.
[2].  Wang, H. and C. Yan, A small-molecule p53 activator induces apoptosis through inhibiting MDMX expression in breast cancer cells. Neoplasia, 2011. 13(7): p. 611-9.
[3].   Roh, J.L., J.Y. Park, and E.H. Kim, XI-011 enhances cisplatin-induced apoptosis by functional restoration of p53 in head and neck cancer. Apoptosis, 2014. 19(11): p. 1594-602.