NSC 66811 |
| Catalog No.GC13687 |
A potent inhibitor of Mdm2-p53 interaction
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6964-62-1
Sample solution is provided at 25 µL, 10mM.
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NSC 66811 is a small-molecule inhibitor of the murine double minute 2 (MDM2) p53 interaction with Ki value of 120nM [1].
The N-terminus of p53 and a deep hydrophobic cleft in MDM2 form a short helix between p53 and MDM2. NSC 66811 binds the active site of this cleft. NSC 66811 has a high binding affinity with Ki of 120nM and is 56 times more potent than the natural p53 peptide. The stereoisomers of NSC 66811 mimic the three key residues of p53 (Phe19, Trp26, and Leu26), mediating the interaction with MDM2. NSC 66811 is reported to induce the accumulation of p53, MDM2, and p21cip1/waf proteins in the HCT-116 human colon cancer cell line with wild-type p53. However, NSC 66811 has no effect on the levels for p53, MDM2, and p21cip1/waf protein in the isogenic HCT-116 p53 /cell line [1].
References:
[1] Lu Y, Nikolovska-Coleska Z, Fang X, Gao W, Shangary S, Qiu S, Qin D, Wang S. Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy. J Med Chem. 2006 Jun 29;49(13):3759-62.
| Cas No. | 6964-62-1 | SDF | |
| Chemical Name | 7-[anilino(phenyl)methyl]-2-methylquinolin-8-ol | ||
| Canonical SMILES | CC1=NC2=C(C=C1)C=CC(=C2O)C(C3=CC=CC=C3)NC4=CC=CC=C4 | ||
| Formula | C23H20N2O | M.Wt | 340.42 |
| Solubility | ≥ 34 mg/mL in DMSO, ≥ 3.82 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 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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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
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- 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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