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Cat. No. M2578
RITA Structure

NSC 652287

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 80 In stock
10mg USD 130 In stock
50mg USD 500 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 292.37
Formula C14H12O3S2
CAS Number 213261-59-7
Purity >99%
Solubility DMSO 50 mg/mL
Storage at -20°C
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Keywords: RITA, NSC 652287 supplier, p53, inhibitors

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