NSC 146109 hydrochloride
(Synonyms: XI-011) 目录号 : GC15621
An activator of p53
Cas No.:59474-01-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 59474-01-0 | SDF | |
| 别名 | XI-011 | ||
| 化学名 | (10-methylanthracen-9-yl)methyl carbamimidothioate;hydrochloride | ||
| Canonical SMILES | CC1=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 tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.1561 mL | 15.7803 mL | 31.5607 mL |
| 5 mM | 0.6312 mL | 3.1561 mL | 6.3121 mL |
| 10 mM | 0.3156 mL | 1.578 mL | 3.1561 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。