RHPS4
Based on 5 publication(s) in Google Scholar
RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer.
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- 純度: 99.88%
- CAS 番号: 390362-78-4
- 分子式: C23H20F2N2O4S
- 分子量:458.48
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
IC50: 0.33 μM (telomerase in the TRAP assay)[1].
RHPS4 could sensitize tumor cells to anticancer agents that act via disparate mechanisms[1].
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RHPS4 (0.5-1 μM, 15 days) induces a senescent-like growth arrest in MCF-7 cells[1].
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RHPS4 (1 μM, 4 days) induces phosphorylation of H2AX in transformed and tumor cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, MCF-7 vector control, and MCF-7 c81 cells.
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Concentration:0, 0.2, 0.5, or 1 μM.
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Incubation Time:7 days.
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Result:Inhibited cell proliferation.
? In all the other tumor xenografts, RHPS4 treatment produces about 50% (P < 0.001) TWI at the nadir of the effect and, more important, results in a delay of tumor growth of about 15 (M14 and PC3) and 10 (HT29 and H460) days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 male nude (nu/nu) mice, 6–8 weeks old and weighing 22-24 g (H460, CG5 and HT29, PC3 and M14 cancer models)[2].
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Dosage:15 mg/kg.
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Administration:IV, daily for 15 consecutive days.
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Result:Active as a single agent on all the tumors analyzed. CG5 breast xenografts resulted in the most sensitive tumor.
化学情報
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CAS 番号 390362-78-4
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性状 Solid
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分子量 458.48
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分子式 C23H20F2N2O4S
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Color Brown to reddish brown
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SMILES
O=S([O-])(OC)=O.FC1=CC=C2C(C3=[N+](C)C4=C(C=C(C=C4)F)C5=C3C(N2C)=CC(C)=C5)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nucleic Acids Res
A subcellular selective APEX2-based proximity labeling used for identifying mitochondrial G-quadruplex DNA binding proteins. [Abstract]2024 Dec 24:gkae1259. PMID: 39718986 -
J Exp Med
Inhibition of hTERT/telomerase/telomere mediates therapeutic efficacy of osimertinib in EGFR mutant lung cancer. [Abstract]2024 Nov 4;221(11):e20240435. PMID: 39297884 -
Br J Pharmacol
A mitochondria-targeting and G-quadruplex structure-binding ligand inducing calcium overload and ferroptosis in human cancer cells. [Abstract]2025 Aug;182(16):3923-3951. PMID: 40344208 -
J Chem Inf Model
2025 Jun 9;65(11):5718-5729. PMID: 40366258 -
溶剤 & 溶解度
DMSO : 1 mg/mL (2.18 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (10.91 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jennifer C Cookson, et al. Pharmacodynamics of the G-quadruplex-stabilizing telomerase inhibitor 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4) in vitro: activity in human tumor cells correlates with telomere length and can be enhanced, or antagonized, with cytotoxic agents. Mol Pharmacol. 2005 Dec;68(6):1551-8. [Content Brief]
[2]. Erica Salvati, et al. Telomere damage induced by the G-quadruplex ligand RHPS4 has an antitumor effect. J Clin Invest. 2007 Nov;117(11):3236-47. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1811 mL | 10.9056 mL | 21.8112 mL | 54.5280 mL |