keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
7ACC1 (D 142) 抑制表达MCT1和MCT4肿瘤细胞的乳酸涌入,能选择性干扰肿瘤微环境乳酸通量。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 139 | 现货 | ||
10 mg | ¥ 188 | 现货 | ||
25 mg | ¥ 298 | 现货 | ||
50 mg | ¥ 428 | 现货 | ||
100 mg | ¥ 622 | 现货 | ||
200 mg | ¥ 997 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 683 | 现货 |
产品描述 | 7ACC1 (D 142) selectively affects a single part of the MCT symporter translocation cycle, leading to strict inhibition of lactate influx. This singular activity is associated with antitumor effects less prone to resistance and side effects. |
体外活性 | 7-(Diethylamino)coumarin-3-carboxylic acid compounds on lactate influx using oxidative cancer cells known to maintain in vitro their capacity to take up lactate as an energetic fuel, and the lack of effects on lactate efflux using highly glycolytic cells. Accordingly, in oxidative human cancer cervix cells, SiHa and Hela, which express both MCT1 and MCT4 isoforms, a potent inhibition of both lactate influx and cell proliferation was obtained with 7-(Diethylamino)coumarin-3-carboxylic acid, whereas the bona fide MCT1/MCT2 inhibitor AR-C155858 failed to do so. The effects of 7-(Diethylamino)coumarin-3-carboxylic acid were confirmed in MCT1/4-expressing pharynx squamous FaDu tumor cells. These observations strongly suggest that 7-(Diethylamino)coumarin-3-carboxylic acid compounds are inhibitors of lactate entry through both MCT1 and MCT4 preventing any compensatory effects when MCT1, the main path for lactate uptake, is inhibited. |
体内活性 | 7-(Diethylamino)coumarin-3-carboxylic acid developed to selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment.?The pharmacologic properties of two compounds of this family, including their effects on lactate influx and efflux and antitumor activity, were investigated using human cancer cell lines and mouse xenograft models.?Contrary to the reference MCT1 inhibitor AR-C155858, 7-(Diethylamino)coumarin-3-carboxylic acid unexpectedly inhibited lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.?7-(Diethylamino)coumarin-3-carboxylic acid delayed the growth of cervix SiHa tumors, colorectal HCT116 tumors, and orthoptopic MCF-7 breast tumors.?MCT target engagement was confirmed by the lack of activity of 7-(Diethylamino)coumarin-3-carboxylic acid on bladder UM-UC-3 carcinoma that does not express functional MCT.7-(Diethylamino)coumarin-3-carboxylic acid?also inhibited SiHa tumor relapse after treatment with cisplatin.?Finally, we found that contrary to AR-C155858, 7-(Diethylamino)coumarin-3-carboxylic acid did not prevent the cell entry of the substrate-mimetic drug 3-bromopyruvate (3BP) through MCT1, and contributed to the inhibition of tumor relapse after 3BP treatment. |
细胞实验 | Cervix cancer cells(SiHa and HeLa) and mammary cancer cells (MDA-MB-231, MCF-7) were cultured in Dulbecco's Modified Eagle Medium (DMEM), and HCT-116 colorectal cancer cells in McCoy's 5A medium, UM-UC-3 bladder transitional cell carcinoma and pharynx squamous carcinoma FaDu cells in Eagle's MEM, HL-60 acute promyelocytic leukemia cells and K562 chronic myelogenous leukemia cells were cultured in suspension in RPMI-1640 medium. For treatments, SiHa, Hela, and MDA-MB231 cells were seeded in flat-bottom 96-well plates in DMEM. After overnight incubation, the culture medium was replaced by 100 μL of medium containing 7ACC1, 7ACC2, AR-C155858, or 3BP. Nonadherent HL-60 and K562 cells were directly treated in flat-bottom 96-well plates in RPMI medium. Antiproliferative effects were determined using MTT or Presto Blue assay for adherent cells or cell counting using a Cellometer Auto T4 for nonadherent cells. |
动物实验 | Eight-week-old NMRI female nude mice (Elevage Janvier) were injected subcutaneously with 2 × 106 SiHa cells, 2 × 10^6 HCT-11^6 cells, or 5 × 10^6 UM-UC-3 cells. An orthotopic breast cancer model was also used with MCF-7 tumor cells injected into the mammary fat pad of mice; a 17β-estradiol pellet had first been subcutaneously implanted in these mice as previously described . When tumors reached a mean diameter of 5 mm, 7-(Diethylamino)coumarin-3-carboxylic acid compounds (3 mg/kg) or AR-C155858 (3 mg/kg) were daily injected intraperitoneally; in some experiments, 7-(Diethylamino)coumarin-3-carboxylic acid treatment was combined with cisplatin (5 mg/kg) injected intraperitoneally at days 0 and 7 (7-(Diethylamino)coumarin-3-carboxylic acid administered daily except at days 0 and 7) or 3BP(3 mg/kg) injected i.p. from day 0 to 4 and day 7 to 11 (7-(Diethylamino)coumarin-3-carboxylic acid administered together with 3BP). Cisplatin and 3BP were also administered alone and control mice were injected with vehicle (dimethyl sulfoxide). Tumor sizes were tracked with an electronic calliper and determined using the formula: (length × width^2 × π)/6. |
别名 | DEAC, 香豆素D1421, Coumarin D 1421, 7-(二乙胺基)-2-氧代-2-苯并吡喃-3-羧酸, 7-(Diethylamino)coumarin-3-carboxylic acid, D 1421 |
分子量 | 261.27 |
分子式 | C14H15NO4 |
CAS No. | 50995-74-9 |
keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32 mg/mL (122.48 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.8275 mL | 19.1373 mL | 38.2746 mL | 95.6865 mL |
5 mM | 0.7655 mL | 3.8275 mL | 7.6549 mL | 19.1373 mL | |
10 mM | 0.3827 mL | 1.9137 mL | 3.8275 mL | 9.5686 mL | |
20 mM | 0.1914 mL | 0.9569 mL | 1.9137 mL | 4.7843 mL | |
50 mM | 0.0765 mL | 0.3827 mL | 0.7655 mL | 1.9137 mL | |
100 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9569 mL |
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。
7ACC1 50995-74-9 Membrane transporter/Ion channel Monocarboxylate transporter 7ACC-1 DEAC Inhibitor D1421 inhibit Coumarin D1421 香豆素D1421 Coumarin D 1421 D-1421 Coumarin D-1421 7-(二乙胺基)-2-氧代-2-苯并吡喃-3-羧酸 7-(Diethylamino)coumarin-3-carboxylic acid Monocarboxylate Transporter D 1421 inhibitor