Benproperine phosphate 是一种具有口服活性的,有效的肌动蛋白相关蛋白 2/3 复合亚基 2 (ARPC2) 抑制剂。Benproperine phosphate 通过削弱 Arp2/3 功能来减弱肌动蛋白的聚合反应速率。Benproperine phosphate 有潜力用于止咳,并可以抑制癌细胞迁移和肿瘤转移。
生物活性 | Benproperine phosphate is an orally active, potentactin-related protein 2/3 complex subunit 2 (ARPC2)inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppressescancercell migration and tumor metastasis[1]. |
体外研究 (In Vitro) | Benproperine phosphate (20-120 μM; for 24 hours) inhibits cell viability in a dose-dependent manner[1]. Benproperine phosphate (10 μM; for 24 hours) significantly inhibits the migration of various types of cancer cells and inhibits the migration and invasion of DLD-1, AsPC-1 cells with IC50values of 1-2 μM. Benproperine phosphate (10 μM; for 24 hours) does not affect cortactin-rich lamellipodium in MCF-10A cells[1].
Cell Viability Assay[1] Cell Line: | DLD-1, AsPC-1, CFPAC-1, A375P, A375P, MDA-MB-231, DU145, DU145 cancer cells | Concentration: | 20, 40, 60, 80, 100, 120 μM | Incubation Time: | For 24 hours | Result: | Inhibited cell viability in a dose-dependent manner. |
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体内研究 (In Vivo) | Benproperine phosphate (50, 100 mg/kg; oral gavage; 5 days per week for 4 weeks) inhibits primary pancreatic tumor growth[1]. Benproperine phosphate shows a marked decrease in the lung metastasis of AsPC-1 cells (56.1% inhibition) in mouse. Benproperine phosphate significantly suppressed the liver metastasis of HCT-116 cells by 78.9% and DLD-1 cells by 78.2%[1].
Animal Model: | Female BALB/c nude mice of 6-week-old with AsPC-1 cells[1] | Dosage: | 50, 100 mg/kg | Administration: | Oral gavage; 5 days per week for 4 weeks | Result: | Inhibited primary pancreatic tumor growth compared to the vehicle control (47.7% inhibition) without body weights change. |
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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 : 250 mg/mL(613.59 mM;Need ultrasonic) H2O : ≥ 100 mg/mL(245.43 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.4543 mL | 12.2717 mL | 24.5435 mL | 5 mM | 0.4909 mL | 2.4543 mL | 4.9087 mL | 10 mM | 0.2454 mL | 1.2272 mL | 2.4543 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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