RHPS4

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RHPS4  纯度: 98.62%

RHPS4 是有效的端粒酶 (telomerase) 抑制剂 (IC50 = 0.33 μM)。RHPS4 是 DNA 损伤的诱导剂。

RHPS4

RHPS4 Chemical Structure

CAS No. : 390362-78-4

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5 mg ￥750 In-stock
10 mg ￥1200 In-stock
25 mg ￥2400 In-stock
50 mg ￥4000 In-stock
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RHPS4 相关产品

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  • Bioactive Compound Library Plus

生物活性

RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer[1][2].

IC50 & Target

IC50: 0.33 μM (telomerase in the TRAP assay)[1].
体外研究
(In Vitro)

RHPS4 could sensitize tumor cells to anticancer agents that act via disparate mechanisms[1].
RHPS4 (0.5-1 μM, 15 days) induces a senescent-like growth arrest in MCF-7 cells[1].
RHPS4 (1 μM, 4 days) induces phosphorylation of H2AX in transformed and tumor cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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[2].
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].

上海金畔生物科技有限公司 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)[2].
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.

分子量

458.48

Formula

C23H20F2N2O4S
CAS 号

390362-78-4
运输条件

Room temperature in continental US; may vary elsewhere.
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)
溶解性数据
In Vitro: 

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 — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

    [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.

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