香豆素D1421|T5845|TargetMol

價(jià)格	￥99
包裝	100mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:香豆素D1421	英文名稱:7ACC1
CAS:50995-74-9	品牌: TargetMol
產(chǎn)地: 美國	保存條件: keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: ≥95%	產(chǎn)品類別: 抑制劑
貨號: T5845

Product Introduction

Bioactivity

名稱	7ACC1
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.
細(xì)胞實(shí)驗(yàn)	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.
動(dòng)物實(shí)驗(yàn)	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.
體外活性	7-(Diethylamino)coumarin-3-carboxylic acid對乳酸攝入的影響研究發(fā)現(xiàn)，在使用氧化癌細(xì)胞進(jìn)行的實(shí)驗(yàn)中，這些細(xì)胞已知能夠維持其體外乳酸作為能量燃料的攝取能力，而對于高度糖解的細(xì)胞，該化合物對乳酸排出沒有影響。相應(yīng)地，在表達(dá)MCT1和MCT4亞型的氧化人類宮頸癌細(xì)胞SiHa和Hela中，7-(Diethylamino)coumarin-3-carboxylic acid顯著抑制了乳酸攝入和細(xì)胞增殖，而公認(rèn)的MCT1/MCT2抑制劑AR-C155858未能如此。7-(Diethylamino)coumarin-3-carboxylic acid 在表達(dá)MCT1/4的咽部鱗狀FaDu腫瘤細(xì)胞中的效果得到了確認(rèn)。這些觀察結(jié)果強(qiáng)烈表明，7-(Diethylamino)coumarin-3-carboxylic acid 通過MCT1和MCT4抑制乳酸的進(jìn)入，抑制MCT1（乳酸攝取的主要途徑），防止了任何補(bǔ)償性效應(yīng)。
體內(nèi)活性	7-(Diethylamino)coumarin-3-carboxylic acid被設(shè)計(jì)用于選擇性干擾富含乳酸的腫瘤微環(huán)境中的乳酸流動(dòng)。該化合物家族的兩種化合物的藥理特性，包括其對乳酸進(jìn)出口和抗腫瘤活性的影響，通過使用人類癌癥細(xì)胞系和小鼠異種移植模型進(jìn)行了研究。7-(Diethylamino)coumarin-3-carboxylic acid意外地抑制了表達(dá)MCT1和MCT4轉(zhuǎn)運(yùn)蛋白的腫瘤細(xì)胞中的乳酸進(jìn)口，但不抑制乳酸出口。7-(Diethylamino)coumarin-3-carboxylic acid延緩了宮頸SiHa腫瘤、結(jié)腸HCT116腫瘤和原位MCF-7乳腺腫瘤的生長。通過不表達(dá)功能性MCT的膀胱UM-UC-3癌細(xì)胞缺乏活性，確認(rèn)了MCT目標(biāo)的結(jié)合。7-(Diethylamino)coumarin-3-carboxylic acid還抑制了使用順鉑治療后SiHa腫瘤的復(fù)發(fā)。最后，我們發(fā)現(xiàn)，與AR-C155858不同，7-(Diethylamino)coumarin-3-carboxylic acid沒有阻止底物模擬藥物3-溴丙酸（3BP）通過MCT1進(jìn)入細(xì)胞，并有助于在3BP治療后抑制腫瘤復(fù)發(fā)。
存儲(chǔ)條件	keep away from direct sunlight \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 32 mg/mL (122.48 mM)
關(guān)鍵字	7ACC-1 \| Inhibitor \| D1421 \| inhibit \| 7ACC1 \| Coumarin D1421 \| D-1421 \| Coumarin D-1421 \| Monocarboxylate Transporter
相關(guān)產(chǎn)品	D-Phenylalanine \| 7ACC2 \| AZD3965 \| VB124 \| AR-C155858 \| Niflumic acid \| MSC-4381 \| α-Cyano-4-hydroxycinnamic acid \| BAY-8002 \| MCT1-IN-3 \| AZD0095 \| Coumarin343
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 抗癌化合物庫 \| 已知活性化合物庫 \| NO PAINS 化合物庫 \| 離子通道庫 \| 膜蛋白靶向化合物庫 \| 表型篩選靶點(diǎn)鑒定庫

關(guān)鍵字：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

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

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