RITA

Item no.	S2781-10
Manufacturer	Selleckchem
CASRN	213261-59-7
Amount	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 5 mg 50 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Testicular & Prostate Cancer
Type	Inhibitors
Specific against	other
Smiles	C1=C(SC(=C1)C2=CC=C(O2)C3=CC=C(S3)CO)CO
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	NSC 652287
Similar products	RITA
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	292, 37
Administration	Administered via i.v. or i.p.
Animal Models	SCID mice carrying HCT116 and HCT116 TP53-/- xenografts
Cell lines	HCT116 cells and HCT116 TP53-/- cells
Concentrations	0.1 nM - 1 mM, 10 mM stocked in DMSO
Dosages	0.1 mg/kg, 1 mg/kg or 10 mg/kg
Formulation	Phosphate buffered saline
IC50	2 nM, 2 nM, 2 nM, 2 nM, 2 nM, 2 nM
In vitro	RITA shows a highly selective pattern of differential cytotoxic activity in the tumor cell lines, due to cellular accumulation to the cytosolic (S100) fraction. RITA also inhibits the growth of other renal cell lines including ACHN and UO-31 with IC50 of 13 uM and 37 uM, respectively. [1] RITA (10 nM) causes cell cycle arrest with accumulation of cells at the G2-M phase and induces DNA fragmentation and apoptosis at 100 nM, both with evaluated p53 protein levels. RITA (30 nM) also induces both DNA-protein and DNA-DNA cross-links in A498 cells. Meanwhile RITA has no effects on top1-mediated relaxation of supercoiled SV40 DNA. [2] RITA significantly suppresses the growth of HCT116 cells (97%) but only slightly inhibits the growth of HCT116 TP53-/- cells (13%). RITA is much more efficient at growth suppression in wild-type p53-expressing tumor cell lines than in cell lines lacking p53 and those expressing mutant p53. RITA binds full-length p53 but not glutathione S-transferase (GST) protein or HDM-2 (a key regulator of p53 is strongly supported by the rescue of embryonic lethality of MDM2). RITA blocks p53 HDM-2 interaction and p53 ubiquitination. RITA substantially decreases the amount of HDM-2 that is co-precipitated with p53, although both proteins are upregulated. RITA prevents interactions between the purified GST-p53 and 6XHis-tagged His-HDM-2 proteins. [3] RITA is shown to induce apoptosis by promoting p53Ser46 phosphorylation. [4] RITA induces activation of p53 in conjunction with up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. RITA induces the activation of JNK signaling. [5] But On the contrary, another results by nuclear magnetic resonance (NMR) show that RITA does not block the formation of the complex between p53 (residues 1-312) and the N-terminal p53-binding domain of MDM2 (residues 1-118), which is highly probable that the binding of RITA requires native conformation of p53. [6]
In vivo	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. Five 1 mg/kg injections of RITA results in a more than twofold decrease in the growth rate of p53-positive xenografts without any effect on p53-null xenografts. 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. [3]
Incubation Time	48 hours
Method	Examination to assess susceptibility of cells to RITA (0.1 nM - 1 mM) is done using the XTT assay. Cells are inoculated into 96-well flat-bottom plates at a density of 1500 cells per well and incubated for 24 hours at 37 C in a humidified 5% CO2 5% air atmosphere. Serial concentrations of RITA in DMSO are added to the wells, and sensitivity is determined 48 hours after the addition of RITA.
Solubility (25C)	DMSO 58 mg/mL, Water <1 mg/mL, Ethanol 8 mg/mL
Information	RITA 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.
Chemical Name	2-Thiophenemethanol, 5, 5'-(2, 5-furandiyl)bis-
Features	Inducer of DNA cross-links, Not DNA intercalator

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