香豆素D1421|T5845|TargetMol

7ACC1
50995-74-9

￥99 100mg 起订

上海更新日期：2024-09-24

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 香豆素D1421

英文名称：: 7ACC1

CAS号：: 50995-74-9

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T5845

Product Introduction

Bioactivity

Name	7ACC1
Description	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.
Cell Research	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.
Animal Research	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.
In vitro	7-(Diethylamino)coumarin-3-carboxylic acid对乳酸摄入的影响研究发现，在使用氧化癌细胞进行的实验中，这些细胞已知能够维持其体外乳酸作为能量燃料的摄取能力，而对于高度糖解的细胞，该化合物对乳酸排出没有影响。相应地，在表达MCT1和MCT4亚型的氧化人类宫颈癌细胞SiHa和Hela中，7-(Diethylamino)coumarin-3-carboxylic acid显著抑制了乳酸摄入和细胞增殖，而公认的MCT1/MCT2抑制剂AR-C155858未能如此。7-(Diethylamino)coumarin-3-carboxylic acid 在表达MCT1/4的咽部鳞状FaDu肿瘤细胞中的效果得到了确认。这些观察结果强烈表明，7-(Diethylamino)coumarin-3-carboxylic acid 通过MCT1和MCT4抑制乳酸的进入，抑制MCT1（乳酸摄取的主要途径），防止了任何补偿性效应。
In vivo	7-(Diethylamino)coumarin-3-carboxylic acid被设计用于选择性干扰富含乳酸的肿瘤微环境中的乳酸流动。该化合物家族的两种化合物的药理特性，包括其对乳酸进出口和抗肿瘤活性的影响，通过使用人类癌症细胞系和小鼠异种移植模型进行了研究。7-(Diethylamino)coumarin-3-carboxylic acid意外地抑制了表达MCT1和MCT4转运蛋白的肿瘤细胞中的乳酸进口，但不抑制乳酸出口。7-(Diethylamino)coumarin-3-carboxylic acid延缓了宫颈SiHa肿瘤、结肠HCT116肿瘤和原位MCF-7乳腺肿瘤的生长。通过不表达功能性MCT的膀胱UM-UC-3癌细胞缺乏活性，确认了MCT目标的结合。7-(Diethylamino)coumarin-3-carboxylic acid还抑制了使用顺铂治疗后SiHa肿瘤的复发。最后，我们发现，与AR-C155858不同，7-(Diethylamino)coumarin-3-carboxylic acid没有阻止底物模拟药物3-溴丙酸（3BP）通过MCT1进入细胞，并有助于在3BP治疗后抑制肿瘤复发。
Storage	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 32 mg/mL (122.48 mM)
Keywords	7ACC-1 \| Inhibitor \| D1421 \| inhibit \| 7ACC1 \| Coumarin D1421 \| D-1421 \| Coumarin D-1421 \| Monocarboxylate Transporter
Inhibitors Related	D-Phenylalanine \| 7ACC2 \| AZD3965 \| VB124 \| AR-C155858 \| Niflumic acid \| MSC-4381 \| BAY-8002 \| MCT1-IN-3 \| AZD0095
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Anti-Cancer Compound Library \| Bioactive Compounds Library Max \| NO PAINS Compound Library \| Ion Channel Targeted Library \| Membrane Protein-targeted Compound Library \| Target-Focused Phenotypic Screening Library

香豆素D1421|||DEAC|||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|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子