Description
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. 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. Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 1036069-26-7
Molecular Weight: 305.80
Formula: C11H12ClNO3S2
Chemical Name: 2-(4,5-dihydro-1,3-thiazol-2-ylsulfanyl)-1-(3,4-dihydroxyphenyl)ethan-1-one hydrochloride
Smiles: Cl.OC1C=C(C=CC=1O)C(=O)CSC1=NCCS1
InChiKey: ZZAVDVMJZKDBIB-UHFFFAOYSA-N
InChi: InChI=1S/C11H11NO3S2.ClH/c13-8-2-1-7(5-9(8)14)10(15)6-17-11-12-3-4-16-11;/h1-2,5,13-14H,3-4,6H2;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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