Powder: -20°C for 3 years | In solvent: -80°C for 1 year
β-Lapachone (ARQ-501) 是一种萘醌类天然产物,是拓扑异构酶 I 抑制剂,通过抑制细胞周期进程来诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 148 | 现货 | ||
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 493 | 现货 | ||
25 mg | ¥ 891 | 现货 | ||
50 mg | ¥ 1,450 | 现货 | ||
100 mg | ¥ 2,280 | 现货 | ||
200 mg | ¥ 3,380 | 现货 | ||
500 mg | ¥ 5,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 318 | 现货 |
产品描述 | β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase. |
靶点活性 | IDO1:0.44 μM |
体外活性 | Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. [1] Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. [2] Beta-Lapachone facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. [3] In addition, beta-Lapachone inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and beta-lapachone also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. [4] Beta-lapachone induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation. [5] |
体内活性 | Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of beta-lapachone and taxol produces a synergistic induction of apoptosis. [6] In normal and diabetic (db/db) mice, treatment of beta-lapachone results in a faster healing process than vehicle only. [3] |
激酶实验 | Topoisomerase I Catalytic Actioity Assay [1]: Topoisomerase I Catalytic Actioity Assay: The enzymatic activity is analyzed by the DNA unwinding assay. DNA topoisomerase I, from TopoGEN (1 unit, which is defined as the amount of enzyme that converts 0.5 μg of superhelical DNA to the relaxed state in 30 minutes at 37 °C), is incubated with 0.5 μg of 6x174 RF DNA, in the presence or absence of Beta-Lapachone, in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCI, 10 mM MgCl2, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 minutes at 37 °C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-hour incubation at 37 °C, the products are separated by electrophoresis in 1% agarose gel in TAE buffer (0.04 M tris acetate, 0.001 M EDTA). The gel is stained with ethidium bromide after electrophoresis. The photographic negative is scanned with an NIH image analysis system. |
细胞实验 | IC50 calculations for each cell line are determined by DNA amount (IS) and anchorage-dependent colony formation (CF) assays. For the CF assay, cells are seeded at 500 viable cells/well in 6-well plates and incubated overnight, then treated with equal volumes of media containing beta-lapachone at final concentrations ranging from 0.005 to 50 μM in half-log increments (controls were treated with 0.25% DMSO, equivalent to the highest dose of beta-lapachonc used) for 4 hour or for continuous 12-hour exposures. Plates (3 wells/condition) are stained with crystal violet, and colonies of >50 normal-appearing cells are enumerated. IC50 values for various cells are calculated using drug doses with numbers of colonies surrounding 50% of control. For DNA assays, plates are harvested for IC50 determinations 8 days after treatment using a CytoFluor 2350 fluorescence measurement system. Six-well samplings are included in the calculation of DNA fluor units for each dose. A graph of beta-lapachone dose versus percentage control DNA in fluor units is used to calculate each IC50. All experiments are repeated at least twice, each in duplicate. (Only for Reference) |
别名 | 3,4-二氢-2,2-二甲基-2H-萘并[1,2-B]吡喃-5,6-二酮, Beta-Lapachone, NSC-26326, SL-11001, ARQ-501 |
分子量 | 242.27 |
分子式 | C15H14O3 |
CAS No. | 4707-32-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 12.1 mg/mL (50 mM)
DMSO: 24.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 4.1276 mL | 20.6381 mL | 41.2763 mL | 103.1907 mL |
5 mM | 0.8255 mL | 4.1276 mL | 8.2553 mL | 20.6381 mL | |
10 mM | 0.4128 mL | 2.0638 mL | 4.1276 mL | 10.3191 mL | |
20 mM | 0.2064 mL | 1.0319 mL | 2.0638 mL | 5.1595 mL | |
50 mM | 0.0826 mL | 0.4128 mL | 0.8255 mL | 2.0638 mL | |
DMSO | 100 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0319 mL |
中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
吊灯树 | Kigelia africana | - | ― | |
木蝴蝶 | Oroxylum indicum(L.)Vent. | 凉 | 苦, 甘 | 肺, 肝, 胃 |
中成药名称 | 处方组成 | 主治疾病 | 中成药类型 |
金嗓利咽丸 | 茯苓,法半夏,枳实,青皮,胆南星,橘红,砂仁,豆蔻,槟榔,合欢皮,六神曲,紫苏梗,生姜,蝉蜕,木蝴蝶,厚朴 | 口服,大蜜丸一次1~2丸,水蜜丸60~120粒(6克~12克),一日2次。 | 燥湿药 |
金嗓开音片 | 金银花,连翘,黄芩,板蓝根,赤芍,玄参,菊花,牛蒡子,木蝴蝶,胖大海,僵蚕(麸炒),蝉蜕 | 口服。一次3片,一日2次。 | 清热药 |
金嗓开音丸 | 金银花,加翘,玄参,板蓝根,赤芍,黄芩,桑叶,菊花,前胡,苦杏仁,牛蒡子,泽泻,胖大海,僵蚕,蝉蜕,木蝴蝶 | 口服,大蜜丸一次1~2丸,水蜜丸60~120粒(6克~12克),一日2次。 | 化痰药 |
金嗓清音颗粒 | 玄参,麦冬,地黄,丹皮,赤芍,黄芩,川贝母,石斛,僵蚕(麸炒),薄荷,木蝴蝶,甘草 | N/A | 清热药 |
菊梅利咽含片 | 马勃,木蝴蝶,菊花,乌梅 | 口含服,一次1片,一日6次。 | 化痰、止咳、平喘药 |
金嗓清音片 | 玄参,麦冬,生地黄,牡丹皮,赤芍,黄芩,川贝母,石斛,僵蚕(麸炒),薄荷,木蝴蝶,甘草 | 口服。一次3片,一日2次。 | 清热药 |
金嗓清音胶囊 | 玄参,麦冬,地黄,丹皮,赤芍,黄芩,川贝母,石斛,薄荷,木蝴蝶,甘草 | 口服,一次3粒,一日2次。 | 清热药 |
广东凉茶 | 岗梅,木蝴蝶,淡竹叶,金沙藤,火炭母,王指柑,金樱根,布渣叶,山芝麻,广金钱草 | 泡服,一次2袋,一日2次。 | 解表药 |
金嗓利咽片 | 茯苓,法半夏,枳实(炒),青皮(炒),胆南星,橘红,砂仁,豆蔻,槟榔,合欢皮,六神曲(炒),紫苏梗,生姜,蝉蜕,木蝴蝶,厚朴(制) | 口服,一日2次,一次2粒。 | 燥湿药 |
金嗓散结颗粒 | 金银花,板蓝根,玄参,蒲公英,木蝴蝶,浙贝母,蝉蜕,马勃,丹参,红花 | 开水冲服。一次1~2袋,一日2次。 | 清热药 |
金嗓开音颗粒 | 金银花,连翘,黄芩,板蓝根,赤芍,玄参,菊花,牛蒡子,木蝴蝶,胖大海,僵蚕(麸炒),蝉蜕 | 开水冲服。一次1袋,一日2次。 | 清热药 |
杏贝止咳颗粒 | 麻黄(炙),苦杏仁,桔梗,前胡,浙贝母,百部,北沙参,木蝴蝶,甘草 | 开水送服,一次1袋,一日3次。疗程7天。 | 化痰、止咳、平喘药 |
咽炎胶囊 | 玄参,板蓝根,天冬,麦冬,牡丹皮,百部(制),青果,款冬花(制),木蝴蝶,地黄,蝉蜕,薄荷油 | 口服,一次4粒,一日3次。 | 清热药 |
金嗓散结片 | 金银花,板蓝根,玄参,蒲公英,木蝴蝶,浙贝母,蝉蜕,马勃,丹参,红花 | 口服,一次2~4片,一日2次。 | 清热药 |
金嗓开音胶囊 | 金银花,连翘,黄芩,板蓝根,赤芍,玄参,菊花,牛蒡子,木蝴蝶,胖大海,僵蚕(麸炒),蝉蜕 | 一次3粒,一日2次。 | 清热药 |
金菊利咽口含片 | 马勃,金银花,菊花,玄参,桔梗,牡丹皮,木蝴蝶,乌梅,冰片,薄荷脑,目草 | 口含服,一次1片,一日6次。5天为一疗程。 | 清热药 |
金嗓利咽颗粒 | 茯苓,枳实(炒),胆南星,木蝴蝶,法半夏,蝉蜕,橘红,槟榔,厚朴(制),砂仁,豆蔻,紫苏梗 | 开水冲服。一次1~2袋,一日2次。 | 燥湿药 |
金嗓利咽胶囊 | 茯苓,枳实,胆南星,砂仁,槟榔,六神曲,生姜,木蝴蝶,法半夏,青皮,橘红,豆蔻,合欢皮,紫苏梗,蝉蜕,厚朴 | 口服,一次2~4粒,一日2次。 | 化痰药 |
保喉片 | 连翘,木蝴蝶,乌梅,诃子,桔梗,天花粉,甘草,薄荷油,蟾酥,麦冬,党参,玄参,僵蚕,黄芪,百部,冰片 | 含服,每隔 1小时含服 2~3片。 | 燥湿药 |
广东凉茶颗粒 | 岗梅,山芝麻,五指柑,淡竹叶,木蝴蝶,布渣叶,火炭母,金沙藤,广金钱草,金樱根 | 用开水冲服,一次1袋,一日1-2次。 | 化湿药 |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
β-Lapachone 4707-32-8 Apoptosis Autophagy DNA Damage/DNA Repair Metabolism IDO Topoisomerase NSC26326 3,4-二氢-2,2-二甲基-2H-萘并[1,2-B]吡喃-5,6-二酮 b-Lapachone Inhibitor NSC 26326 ARQ501 ARQ 501 Beta-Lapachone NSC-26326 SL-11001 β Lapachone inhibit βLapachone ARQ-501 SL 11001 SL11001 inhibitor