| CAS NO: | 1036069-26-7 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1036069-26-7 |
| 化学名 | 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 |
| 分子式 | C11N11NO3S2 |
| 分子量 | 305.8 |
| 溶解度 | <30.58mg/ml in DMSO |
| 储存条件 | Desiccate at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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