[CAS NO. 213261-59-7]  RITA

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PRODUCTS SPECIFICATIONS [213261-59-7]

Catelog
HY-13424
Brand
MCE
CAS
213261-59-7

DESCRIPTION [213261-59-7]

Overview

MDLMFCD03235294
Molecular Weight292.37
Molecular FormulaC14H12O3S2
SMILESOCC1=CC=C(C2=CC=C(C3=CC=C(CO)S3)O2)S1

For research use only. We do not sell to patients.


Summary

RITA is an inhibitor of p53-HDM-2 interaction , binds to p53dN, with a K d of 1.5 nM, and also induces DNA-DNA cross-links .


IC50 & Target

Kd: 1.5 nM (p53dN) [1]
DNA Crosslinker [2]


In Vitro

RITA inhibits p53-HDM-2 interaction, binding to p53dN, with a K d of 1.5 nM. RITA (10 μM) blocks complex formation between p53 and HDM-2 in HCT116 cells and HDFs and in NHF-ERMyc cells irrespective of c-Myc expression. RITA (0.5 μM) reduces the viability of tumor cells in a wild-type p53-dependent manner. Moreover, RITA (0.1 μM) induces p53-dependent apoptosis. RITA induces p53 but does not via DNA damage-signaling pathway [1] . RITA (NSC 652287) induces DNA-DNA cross-links. RITA induces G2-M cell cycle arrest at 10 nM and causes apoptosis at 100 nM. RITA (100 nM) also elevates p53 and causes dose-dependent effects on p 21WAF1 protein levels [2] . RITA inhibits the growth of HeLa and CaSki cells, with IC 50 s of 1 and 10 μM. In addition, RITA (1 μM) stabilizes p53 by inhibiting p53/E6AP interaction [3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

RITA (0.1, 1 or 10 mg/kg, i.p.) shows potent antitumor activity in SCID mice bearing HCT116 and HCT116 TP53 −/− xenografts [1] . RITA (10 mg/kg, i.p.) also suppresses the growth of HeLa cells in SCID mice [3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT05260203 Advice Pharma Group srl
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
June 4, 2022 Not Applicable

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 342.03 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4203 mL 17.1016 mL 34.2032 mL
5 mM 0.6841 mL 3.4203 mL 6.8406 mL
10 mM 0.3420 mL 1.7102 mL 3.4203 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

2-Thiophenemethanol, 5,5′-(2,5-furandiyl)bis-
5,5′-(2,5-Furandiyl)bis[2-thiophenemethanol]
NSC 652287
RITA
[Furan-2,5-diylbis(thiene-5,2-diyl)]dimethanol
[5-[5-[5-(Hydroxymethyl)thiophen-2-yl]furan-2-yl]thiophen-2-yl]methanol