PhiKan 083 |
| Catalog No.GC12658 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 880813-36-5
Sample solution is provided at 25 µL, 10mM.
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Ki: ≈ 150 M
PhiKan 083 is a critical p53 stabilizing agent by bonding its mutation Y220C
The mutation Y220C of p53 exists a surface cavity that destabilizes the protein by 4 kcal/mol, at a site that is not functional. A p53 stabilizing agent binding it is able to slow rate of thermal denaturation [1].
In vitro: Isothermal titration of PhiKan083 with T-p53C-Y220C exhibited 1:1 stoichiometry and a Kd of 125 ± 10 M. PhiKan083 stabilized T-p53C-Y220C in a concentration-dependent manner. In a simple binding model for PhiKan083 (T-p53C-Y220C at 310 K (37°C)), in the absence of ligand, the protein gave a half-life of 3.8 min, while it increased to 15.7 min at saturating concentrations of PhiKan083. This is a proposed anticancer drug that could be developed for the Y220C mutant using p53 stabilizing agent. The site of mutation in the oncogenic Y220C mutant PhiKan083 binds with reasonable affinity is a druggable target. Interestingly, the site of mutation does not exist in a region of the protein that is functionally important, it will be an excellent target for drug stabilization therapy. This suggests the crystal structure of the complex will be a fresh start for further rounds of drug design and refinement [1].
In vivo: So far, no study in vivo has been conducted.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Boeckler FM, Joerger AC, Jaggi G, Rutherford TJ, Veprintsev DB, Fersht AR. Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29; 105(30):10360-5.
| Cas No. | 880813-36-5 | SDF | |
| Chemical Name | 1-(9-ethyl-9H-carbazol-3-yl)-N-methylmethanamine hydrochloride | ||
| Canonical SMILES | CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.Cl | ||
| Formula | C16H18N2.HCl | M.Wt | 274.79 |
| Solubility | <13.74mg/ml in Water; <27.48mg/ml in DMSO | Storage | Store at 4°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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6391 mL | 18.1957 mL | 36.3914 mL |
| 5 mM | 0.7278 mL | 3.6391 mL | 7.2783 mL |
| 10 mM | 0.3639 mL | 1.8196 mL | 3.6391 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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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