213261-59-7
RITA (NSC 652287)
CAS: 213261-59-7
Molecular Formula: C14H12O3S2
213261-59-7 - Names and Identifiers
| Name | RITA (NSC 652287) |
| Synonyms | RITA (NSC 652287) p53 Activator III 5,5'-(2,5-FURANDIYL)BIS-2-THIOPHENEMETHANOL 2-Thiophenemethanol, 5,5'-(2,5-furandiyl)bis- (5,5'-(furan-2,5-diyl)bis(thiophene-5,2-diyl))diMethanol 5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol NSC 652287 5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol RITA (NSC 652287) NSC 652287 5,5'-(2,5-Furandiyl)bis-2-thiophenemethanol |
| CAS | 213261-59-7 |
| EINECS | 200-256-5 |
213261-59-7 - Physico-chemical Properties
| Molecular Formula | C14H12O3S2 |
| Molar Mass | 292.37 |
| Density | 1.396±0.06 g/cm3(Predicted) |
| Melting Point | 160 °C |
| Boling Point | 464.9±40.0 °C(Predicted) |
| Solubility | Soluble in DMSO (58 mg/ml at 25 °C), ethanol (8 mg/ml at 25 °C), DMF (30 mg/ml), 1: |
| Appearance | Crystalline solid |
| Color | Yellow |
| pKa | 13.43±0.10(Predicted) |
| Storage Condition | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| Stability | Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Sensitive | Light Sensitive |
| Use | A trycyclic thiophene derivative that binds MDM2, activates p53 and induces apoptosis. |
| In vitro study | RITA acts on tumor cells and shows a high selectivity of different toxicities due to the accumulation of cytoplasmic (S100) components. RITA also inhibited other kidney cell lines, including ACHN and UO-31 growth, with IC50 of 13 μm and 37 μm, respectively. RITA (10 nM) arrested the cell cycle, allowed the cells to accumulate in G2-M, induced DNA fragmentation and apoptosis at 100 nM, and increased p53 protein levels. RITA (30 nM) also induced DNA protein and DNA-DNA cross-linking in A498 cells. Meanwhile, RITA had no effect on top1-regulated supercoiled SV40 DNA loosening. RITA significantly inhibited HCT116 cell growth (97%), while slightly inhibited HCT116 TP53. RITA induced apoptosis by promoting phosphorylation of p53Ser46. RITA induces p53 activation with up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. RITA induces activation of JNK signaling. However, in contrast, another result by nuclear magnetic resonance (NMR) showed that RITA did not block p53 (RESIDUES 1-312) and the N-terminal p53 binding domain of MDM2 (RESIDUES 1-118). The formation of a complex between them, which is likely to be the natural idea that the binding of RITA requires p53. |
| In vivo study | The mice were well tolerated by the I. P. Administration of RITA, and no significant weight loss was observed at a dose of 10 mg/kg for 1 month. After 5 injections of 0.1 mg/kg of RITA, the growth of HCT116 tumor was inhibited by 40%, while that of HCT116 TP53 |
213261-59-7 - Risk and Safety
| HS Code | 29321900 |
213261-59-7 - Introduction
RITA (NSC 652287) induces DNA-protein and DNA-DNA cross-linking. DNA single strand breaks cannot be detected. By targeting p53, it also inhibits MDM2-p53 interaction.
Last Update：2022-10-16 17:41:34
213261-59-7 - Reference Information
| biological activity | RITA (NSC 652287) induces DNA-protein and DNA-DNA cross-linking, cannot detect DNA single strand breaks, and also inhibits MDM2-p53 interaction by targeting p53. |
| target | TargetValue Mdm2 p53 () |
| Target | Value |
| In vitro studies | RITA acts on tumor cells and shows a high degree of selectivity for different toxicities because of the accumulation of cytoplasmic (S100) components. RITA also inhibited the growth of other kidney cell lines, including ACHN and UO-31, with IC50 of 13 μM and 37 μM, respectively. RITA (10 nM) stagnates the cell cycle, accumulates cells in G2-M phase, induces DNA fragments and apoptosis when nM is 100, and increases p53 protein level. RITA (30 nM) acts on A498 cells and also induces DNA protein and DNA-DNA crosslinking. At the same time, RITA had no effect on top1-regulated supercoiled SV40 DNA loosening. RITA significantly inhibited HCT116 cell growth (97%), while slightly inhibited HCT116 TP53 RITA induced apoptosis by promoting p53Ser46 phosphorylation. RITA induces p53 activation, accompanied by up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. RITA induces activation of JNK signaling. However, on the contrary, another result by nuclear magnetic resonance (NMR) shows that RITA does not block the formation of complexes between p53 (residues 1-312) and the N-terminal p53 binding domain of MDM2 (residues 1-118), which is likely to be the natural conception that the binding of RITA requires p53. |
| in vivo study | RITA was injected intraperitoneally into mice with good tolerance and no obvious weight loss was observed after treatment at a dose of 10 mg/kg for 1 month. After 5 injections of 0.1 mg/kg RITA, 40% HCT116 tumor growth was inhibited, while HCT116 TP53 |
Last Update：2024-04-09 21:54:55
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Product Name: RITA (NSC 652287) Visit Supplier Webpage Request for quotationCAS: 213261-59-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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