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RHPS4

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

目录号: PC10380 纯度: ≥98%

CAS No. :390362-78-4

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中文名称	RHPS4
中文别名	3,11-二氟-6,8,13-三甲基-8H-喹啉并[4,3,2-kl]吖啶鎓硫酸甲酯盐
英文名称	RHPS4
英文别名	RHPS4
Cas No.	390362-78-4
分子式	C₂₃H₂₀F₂N₂O₄S
分子量	458.48
包装储存	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

RHPS4 is a potent telomerase inhibitor (IC₅₀ = 0.33 μM). RHPS4 is a DNA damage inducer.

性状

Solid

IC50 & Target[1][2]

IC50: 0.33 μM (telomerase in the TRAP assay).

体外研究(In Vitro)

RHPS4 could sensitize tumor cells to anticancer agents that act via disparate mechanisms.
RHPS4 (0.5-1 μM, 15 days) induces a senescent-like growth arrest in MCF-7 cells.
RHPS4 (1 μM, 4 days) induces phosphorylation of H2AX in transformed and tumor cells.

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

Cell Proliferation Assay

Cell Line:	MCF-7, MCF-7 vector control, and MCF-7 c81 cells.
Concentration:	0, 0.2, 0.5, or 1 μM.
Incubation Time:	7 days.
Result:	Inhibited cell proliferation.

体内研究(In Vivo)

RHPS4 (15 mg/kg, iv, 15 days) treatment produces a marked inhibition of tumor weight (tumor weight inhibition [TWI] about 80%; P < 0.001) in a very short time, and this effect persists for at least 30 days. A complete tumor response is observed in 80% of mice, and 40% are cured.
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.

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

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).
Dosage:	15 mg/kg.
Administration:	IV, daily for 15 consecutive days.
Result:	Active as a single agent on all the tumors analyzed. CG5 breast xenografts resulted in the most sensitive tumor.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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) 体外研究: 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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 1 mg/mL (2.18 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1811 mL	10.9056 mL	21.8112 mL
5 mM	---	---	---
10 mM	---	---	---

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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