RETRA hydrochloride |
| Katalog-Nr.GC10589 |
Antitumor agent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1036069-26-7
Sample solution is provided at 25 µL, 10mM.
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IC50: Inhibit tumor cells growth with an IC50of about 4 M.
Being defective for the tumor-suppressor function, mutant p53, a major contributor to malignancy, exerts oncogenic activity also by blocking another tumor-suppressing protein - p73. RETRA hydrochloride is considered to restore mutant p53 activity and therefore to inhibit growth of carcinoma cells. This small molecular could also transcriptionally up-regulates the expression of p53-responsive gene and induces the activation of caspases 3 and 7. RETRA’s anticancer activity is restricted to tumor cells bearing mutant p53. [1]
In vitro: Ewing’s sarcoma (ES) cells with mutant p53 were explored to RETRA, it was found that this compound could substantially up-regulate the expression level of p73 and therefore increase the apoptosis of tumor cells in three mutant p53 ES cell lines. In addition, RETRA was described to activate a set of p53-regulated genes in vitro. However, for most of the p53-deficient carcinoma, osteosarcoma and leukaemia cells, RETRA had no significant effect. [1, 2]
In vivo: Effect of RETRA hydrochloride was studied in vivo using mouse xenografts model. It was noticed that mutant p53-bearing tumor cells were specifically suppressed with a significantly increase in the p73 level and a release of p73 from the blocking complex with mutant p53. [1]
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Kravchenko JE, Ilyinskaya GV, Komarov PG, Agapova LS, Kochetkov DV, Strom E, Frolova EI, Kovriga I, Gudkov AV, Feinstein E, Chumakov PM. Small molecular RETRA suppresses mutant p53-bearing cancer cells through a p73-dependent salvage pathway. PNAS. 2008 Apr; 105(17): 6302–7.
[2] Sonnemann J, Grauel D, Blumel L, Hentschel J, Marx C, Blumrich A, Focke K, Becker S, Wittig S, Schinkel S, Kramer OH, Beck JF. RETRA exerts anticancer activity in Ewing’s sarcoma cells independent of their TP53 status. EUR J CANCER. 2015 Feb; 51:841-851.
| Cas No. | 1036069-26-7 | SDF | |
| Chemical Name | 2-(4,5-dihydro-1,3-thiazol-2-ylsulfanyl)-1-(3,4-dihydroxyphenyl)ethanone;hydrochloride | ||
| Canonical SMILES | C1CSC(=N1)SCC(=O)C2=CC(=C(C=C2)O)O.Cl | ||
| Formula | C11N11NO3S2 | M.Wt | 305.8 |
| Löslichkeit | <30.58mg/ml in DMSO | 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 | 3.2701 mL | 16.3506 mL | 32.7011 mL |
| 5 mM | 0.654 mL | 3.2701 mL | 6.5402 mL |
| 10 mM | 0.327 mL | 1.6351 mL | 3.2701 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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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