Name: RITA
Brand: Selleck Chemicals
SKU: S2781
Availability: InStock
Rating: 5 (13 reviews)

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Quality Control

Batch: S278101 DMSO]58 mg/mL]false]Ethanol]8 mg/mL]false]Water]Insoluble]false Purity: 99.93%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.93

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other p53 Inhibitors	Eprenetapopt (APR-246) CBL0137 Hydrochloride Pifithrin-α (PFTα) Hhydrobromide Pifithrin-μ Serdemetan (JNJ-26854165) PRIMA-1 NSC348884 NSC 319726 (ZMC1) Tenovin-6 Tenovin-1

Solubility

In vitro
Batch:

DMSO : 58 mg/mL (198.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (102.61mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	292.37	Formula	C₁₄H₁₂O₃S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	213261-59-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 652287			Smiles	C1=C(SC(=C1)C2=CC=C(O2)C3=CC=C(S3)CO)CO

Mechanism of Action

Features	Inducer of DNA cross-links, not a DNA intercalator.
Targets/IC₅₀/Ki	Mdm2 p53
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. This compound also inhibits the growth of other renal cell lines including ACHN and UO-31 with IC50 of 13 μM and 37 μM, respectively. It (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. This chemical (30 nM) also induces both DNA-protein and DNA-DNA cross-links in A498 cells. Meanwhile it has no effects on top1-mediated relaxation of supercoiled SV40 DNA. It significantly suppresses the growth of HCT116 cells (97%) but only slightly inhibits the growth of HCT116 TP53^-/- cells (13%). This compound 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. It 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). This chemical blocks p53−HDM-2 interaction and p53 ubiquitination. It substantially decreases the amount of HDM-2 that is co-precipitated with p53, although both proteins are upregulated. This compound prevents interactions between the purified GST-p53 and 6XHis-tagged His-HDM-2 proteins. It is shown to induce apoptosis by promoting p53Ser46 phosphorylation. This chemical induces activation of p53 in conjunction with up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. It induces the activation of JNK signaling. But On the contrary, another results by nuclear magnetic resonance (NMR) show that it 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 this compound requires native conformation of p53.
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 this compound, 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, it shows strong antitumor activity. Five 1 mg/kg injections of this chemical 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 it than in control untreated mice. This compound inhibits the tumor growth in a wild-type p53−dependent manner.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10230772/ [2] https://pubmed.ncbi.nlm.nih.gov/10462535/ [3] https://pubmed.ncbi.nlm.nih.gov/15558054/ [4] https://pubmed.ncbi.nlm.nih.gov/22166212/ [5] https://pubmed.ncbi.nlm.nih.gov/22276160/ [6] https://pubmed.ncbi.nlm.nih.gov/16270059/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05260203	Completed	Multiple Myeloma\|Solitary Plasmacytoma\|Amyloidosis\|Chronic Myeloid Leukemia\|Chronic Lymphocytic Leukemia\|T Cell Non-Hodgkin Lymphoma\|Lymphocytic Lymphoma\|Hodgkin Lymphoma\|B-cell Non Hodgkin Lymphoma\|Acute Myeloid Leukemia\|Myelodysplasia\|Chronic Myeloproliferative Disorder\|Treatment Adherence\|Treatment Adherence and Compliance	Advice Pharma Group srl	June 4 2022	Not Applicable
NCT05153551	Completed	Autism Spectrum Disorder	University of Michigan\|Blue Cross Blue Shield of Michigan Foundation	January 27 2022	Not Applicable
NCT03806127	Completed	Irritable Bowel Syndrome	Urovant Sciences GmbH	December 31 2018	Phase 2
NCT00779025	Completed	Coitus	Johnson & Johnson Consumer and Personal Products Worldwide	January 2008	Not Applicable

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RITA p53 activator

Chemical Structure

Molecular Weight: 292.37