CP 31398 dihydrochloride |
| カタログ番号GC15840 |
p53安定剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1217195-61-3
Sample solution is provided at 25 µL, 10mM.
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CP 31398 dihydrochloride is a potent activator of p53 with maximum tolerated dose of 400 ppm [2].
Tumor protein p53 (p53) is a crucial protein in multicellular organisms and plays an important role in preventing cancer formation. Many studies have shown that activated p53 regulates the expression of p21 which binds to the G1-S/CDK complexes (molecules important for the G1/S transition in the cell cycle) and inhibits their activity [1].
CP 31398 dihydrochloride is a potent p53 stabilization and is regarded as a promising agent which combines with chemotherapy drugs for cancer treatment. When tested with a panel of 9 human cancer cell lines, CP 31398 dihydrochloride treatment resulted in cell apoptosis in mutant or wild-type p53 expressed cell lines (SW480, SKBr3, PA1, U20S, HCT116, and Saos-2) and enhanced chemotherapeutic drugs effect on cell killing while had no effect on cell lines not expressed p53 [1]. In four human HNSCC cell lines (JHU-O29, UMSCC-22A and Fadu), administration of CP 31398 dihydrochloride for 96 h inhibited the cell growth by accumulating p53 expression [2].
In colon adenocarcinomas F344 rast model, combination low dose of CP 31398 dihydrochloride with celecoxib markedly suppressed colon adenocarcinoma incidence (78%) and multiplicity (90%) by enhancing the expression of p53 which indicated that a combination of low dose CP-31398 dihydrochloride and celecoxib could be a promising therapy for colon cancer in clinic [3].
References:
[1]. Takimoto, R., et al., The mutant p53-conformation modifying drug, CP-31398, can induce apoptosis of human cancer cells and can stabilize wild-type p53 protein. Cancer Biol Ther, 2002. 1(1): p. 47-55.
[2]. Roh, J.L., et al., p53-Reactivating small molecules induce apoptosis and enhance chemotherapeutic cytotoxicity in head and neck squamous cell carcinoma. Oral Oncol, 2011. 47(1): p. 8-15.
[3]. Rao, C.V., et al., Inhibition of azoxymethane-induced colorectal cancer by CP-31398, a TP53 modulator, alone or in combination with low doses of celecoxib in male F344 rats. Cancer Res, 2009. 69(20): p. 8175-82.
| Cas No. | 1217195-61-3 | SDF | |
| Chemical Name | (E)-N1-(2-(4-methoxystyryl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine dihydrochloride | ||
| Canonical SMILES | CN(C)CCCNC1=C2C=CC=CC2=NC(/C=C\C3=CC=C(OC)C=C3)=N1.Cl.Cl | ||
| Formula | C22H26N4O.HCl | M.Wt | 435.39 |
| 溶解度 | <43.54mg/ml in DMSO; <43.54mg/ml in Water | Storage | 4°C, protect from light |
| 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. |
||
| 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 | 2.2968 mL | 11.484 mL | 22.9679 mL |
| 5 mM | 0.4594 mL | 2.2968 mL | 4.5936 mL |
| 10 mM | 0.2297 mL | 1.1484 mL | 2.2968 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: >99.00%
- 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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