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RITA

Cat. No. M2578
RITA Structure
Synonym:

NSC 652287

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 33.3  USD37 In stock
5mg USD 58.5  USD65 In stock
10mg USD 99  USD110 In stock
50mg USD 324  USD360 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 292.37
Formula C14H12O3S2
CAS Number 213261-59-7
Purity >99%
Solubility DMSO 48 mg/mL
Storage at -20°C
References

Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation
Carolyn Ying Zhao, et al. Cancer Res. 2010 Apr 15;70(8):3372-81. PMID: 20395210.

Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors
Natalia Issaeva, et al. Nat Med. 2004 Dec;10(12):1321-8. PMID: 15558054.

DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells
W Nieves-Neira, et al. Mol Pharmacol. 1999 Sep;56(3):478-84. PMID: 10462535.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RITA, NSC 652287 supplier, p53, inhibitors

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