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product name RITA (NSC 652287)


Description: RITA (also known as NSC 652287) induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks. RITA, a drug that, like nutlin-3, can  also disrupt the p53/Mdm2 interaction. IC50: 2 nM and 20 nM for A-498 and TK-10, respectively; A series of naturally occurring and synthetic compounds containing one or more thiophene moieties have been tested in the NCI Anticancer Drug Screen and have demonstrated differential antiproliferative activity. Thiophene derivatives as a class exhibit very similar patterns of differential sensitivity, the molecular basis for which is not clear.

Reference: Biochem Pharmacol. 1999 Jun 1;57(11):1283-95.



Molecular Weight (MW)

292.4
Formula

C14H12O3S2
CAS No.

213261-59-7
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 58 mg/mL (198.37 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 8 mg/mL (27.36 mM)
Solubility (In vivo)

30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19415921

General 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.
Animal model SCID mice carrying HCT116 and HCT116 TP53-/- xenografts
Formulation Phosphate buffered saline
Dosages 0.1 mg/kg, 1 mg/kg or 10 mg/kg
Administration i.p or i.v.
Reference [1] Issaeva N, et al. Nat Med. 2004, 10(12), 1321-1328.

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