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RITA (NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53. RITA binds full-length p53 but not glutathione S-transferase (GST) protein or HDM-2. RITA blocks p53−HDM-2 interaction and p53 ubiquitination. RITA substantially decreases the amount of HDM-2 that coprecipitated with p53, although both proteins were upregulated. RITA induces activation of p53 in conjunction with up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. RITA also induces the activation of JNK signaling. RITA is well tolerated in mice after intraperitoneal administration, with no observable weight loss at doses up to 10 mg/kg during 1 month. After five injections of 0.1 mg/kg of RITA, the growth of the HCT116 tumors is suppressed by 40%, without apparent effects on the HCT116 TP53-/- tumors. At a dose of 1 or 10 mg/kg, RITA shows strong antitumor activity. HCT116 tumors are 90% smaller in mice treated with 10 mg/kg of RITA than in control untreated mice. RITA inhibits the tumor growth in a wild-type p53−dependent manner.
J Cancer Res Clin Oncol. 2023 Apr 29.
Apatinib combined with olaparib induces ferroptosis via a p53-dependent manner in ovarian cancer
RITA purchased from AbMole
Zhonghua Xue Ye Xue Za Zhi. 2017 Feb 14;38(2):160-163.
Rita induce acute lymphoblostic leukemia cell apoptosis by activating P53 pathway
RITA purchased from AbMole
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Source | Oncotarget (2017). Figure 1. RITA |
| Method | FACS analysis | |
| Cell Lines | HD-MB03 and DAOY cell | |
| Concentrations | 1 μM | |
| Incubation Time | 48 h | |
| Results | RITA treatment raised the apoptotic fraction in ONS-76 (P = 0.01) and DAOY (P = 0.03) cultures by 5-fold compared to controls, but had no significant effect on UW-228-2 apoptosis |
| Molecular Weight | 292.37 |
| Formula | C14H12O3S2 |
| CAS Number | 213261-59-7 |
| Solubility (25°C) | DMSO 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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