Dofequidar - CAS:129716-58-1

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Dofequidar (Synonyms:1-[4-[2-羟基-3-(5-喹啉基氧基)丙基]-1-哌嗪基]-2,2-二苯基乙酮；多非喹达)

目录号 : KCM10956 CAS No. : 129716-58-1 纯度 : ≥98%

Data Sheet SDS 产品使用指南

Dofequidar is a quinoline derivative and inhibitor of multidrug resistance. It inhibits P-glycoprotein in a photolabeling assay when used at a concentration of 100 μM. Dofequidar (10 μM) increases intracellular accumulation of [H]-vincristine in HL-60R cells endogenously expressing the gene encoding multidrug resistance-associated protein (MRP). It restores susceptibility to vincristine- or doxorubicin-induced cytotoxicity in vincristine-resistant P388, vincristine-resistant K562, and doxorubicin-resistant K562 cells in a concentration-dependent manner. Dofequidar (80 mg/kg twice per day) increases survival in a vincristine-resistant P388 murine leukemia model compared with untreated controls when administered in combination with vincristine .

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect[1][2].

体外研究

In vitro proliferation and drug sensitivity experiments of human small cell lung cancer SBC-3/ADM and SBC-3 cells, Dofequidar showed that 3-10 μM could completely reverse the multidrug resistance of SBC-3/ADM cells to Etoposide (VP-16) Adriamycin, and Vincristine, with little effect on the sensitivity of SBC-3 cells [1].

In the experimental analysis of P-gp expression in human small cell lung cancer SBC-3/ADM and SBC-3 cells, Dofequidar did not alter the expression of P-gp in SBC-3 cells, while SBC-3/ADM cells themselves expressed P-gp [1].

In SP cell sorting experiments of various cancer cell lines, Dofequidar reduced the proportion of side group (SP) cells in a dose-dependent manner [2].

Dofequidar increased the intracellular concentration of ABCC1 ⁄ MDR related protein (MRP) in K562/BCRP cells during intracellular drug accumulation experiments [2].

体内研究

Dofequidar (200 mg/kg; oral; Starting from the 10th or 14th day after inoculation with tumor cells, a total of 4 times, the combination of Etoposide (VP-16) or Adriamycin significantly inhibited the metastasis of SBC-3/ADM cells to multiple organs in a SCID mouse model with NK cell depletion (inoculated with SBC-3/ADM or SBC-3 cells).
Dofequidar (200 mg/kg; oral; Administration of Irinotecan (CPT-11) 30 minutes prior to injection and co administered with Irinotecan on days 0, 4, and 8 significantly reduced tumor volume in a nude mouse model inoculated with HeLa SP cells [2].

Animal Model:	6- to 8-week-old male severe combined immunodeficiency (SCID) mice, depleted of natural killer (NK) cells by intraperitoneal injection of TM-β1 Ab (1 mg/mouse) 2 days before tumor inoculation, and then inoculated intravenously with SBC-3 or SBC-3/ADM cells
Dosage:	200 mg/kg
Administration:	Orally administered; the mice inoculated with SBC-3 cells were treated on days 14, 15, 21, and 22; the mice inoculated with SBC-3/ADM cells were treated on days 10, 11, 17, and 18.
Result:	Combined use with Etoposide (VP-16) (HY-13629) or Adriamycin can significantly inhibit metastasis formation by SBC-3/ADM cells to the liver, kidneys, and lymph nodes, and the weight of the liver of the treated mice was significantly less than that of other groups.

Animal Model:	5- to 6-week-old female BALB/c-nu/nu (nude) mice, inoculated subcutaneously with HeLa SP cells
Dosage:	200 mg/kg
Administration:	Orally administered 30 minutes before intravenous injection of Irinotecan (67 mg/kg); on days 0, 4, and 8
Result:	Co-treatment with Irinotecan drastically decreased the tumor volume.

分子式

C₃₀H₃₁N₃O₃

分子量

481.59

CAS号

129716-58-1

中文名称

1-[4-[2-羟基-3-(5-喹啉基氧基)丙基]-1-哌嗪基]-2,2-二苯基乙酮

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 : 50 mg/mL (103.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0765 mL	10.3823 mL	20.7646 mL
5 mM	0.4153 mL	2.0765 mL	4.1529 mL
10 mM	0.2076 mL	1.0382 mL	2.0765 mL

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 → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.19 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

纯度： ≥98%

Data Sheet

SDS

产品使用指南

[1]. Nokihara H, et al. A new quinoline derivative MS-209 reverses multidrug resistance and inhibits multiorgan metastases by P-glycoprotein-expressing human small cell lung cancer cells. Jpn J Cancer Res. 2001 Jul;92(7):785-92.

[2]. Katayama R, et al. Dofequidar fumarate sensitizes cancer stem-like side population cells to chemotherapeutic drugs by inhibiting ABCG2/BCRP-mediated drug export. Cancer Sci. 2009 Nov;100(11):2060-8.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器