NSC 146109 hydrochloride (Synonyms: XI-011) |
| Catalog No.GC15621 |
An activator of p53
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59474-01-0
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Synonyms | XI-011 | ||
| Chemical Name | (10-methylanthracen-9-yl)methyl carbamimidothioate;hydrochloride | ||
| Canonical SMILES | CC1=C2C=CC=CC2=C(C3=CC=CC=C13)CSC(=N)N.Cl | ||
| Formula | C17H16N2S.HCl | M.Wt | 316.85 |
| Solubility | DMSO: 30 mg/ml,Ethanol: 3 mg/ml | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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