RHPS4
目录号 : KM5333 CAS No. : 390362-78-4 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg 询价 In-stock
200mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

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

体外研究

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.

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

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.

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.
分子式
C23H20F2N2O4S
分子量
458.48
CAS号
390362-78-4
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.25 mg/mL (2.73 mM); Suspended solution; Need ultrasonic

    此方案可获得 1.25 mg/mL (2.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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