| 中文名称： |
盐酸伊达比星 |
| 英文名称: |
Idarubicin hydrochloride |
| 产品分类： |
小分子化合物(化合物库) |
| CAS号： |
57852-57-0 |
| 分子式： |
C26H27NO9.HCL |
| 分子量： |
533.95 |
*产品基础信息：
【产品中文名称】盐酸伊达比星;
【产品英文名称】Idarubicin hydrochloride;
【纯度指标】99.96%;
【品牌】TargetMol;
【CAS号】57852-57-0;
【浓度】;
Product Introduction
Bioactivity
| 名称 | Idarubicin hydrochloride |
| 描述 | Idarubicin hydrochloride (Zavedos), a hydrochloride salt form of Idarubicin, is a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells ( IC50: 3.3 ng/mL). |
| 细胞实验 | The anti-proliferative activity of the Idarubicin in the conjugate is compared to that of free drug by measuring the inhibition of [3H]thymidine uptake. Briefly, NALM-6 cells (1.5 × 106/mL) are added to a flat-bottomed microtitre plate (100 μL/well) and incubated for 1 hours at 37ºC. Free Idarubicin and Idarubicin-mAb conjugates are sterilised by filtration and diluted in sterile PBS; various concentrations are added to the wells (100 μL/well) in duplicate and the plates are incubated at 37ºC, 7% CO2 for 24 hours. Following incubation, 50 μL medium containing 1 μCi [3H]thymidine is added to each well and the plates are incubated for a further 4 hours. Cells are harvested onto glass-fibre filter-paper, dried and counted in a scintillation counter. Specificity studies are performed using the same technique where the ability of Idarubicin-anti-CD19 conjugates to kill CD19 + cells is compared to the cytotoxicity of irrelevant Idarubicin-JGT conjugates. NALM-6 cells (1.5× 106/mL, 300 μL tube) are incubated for 30 rain on ice with various concentrations of Idarubicin-anti-CD 19 or Idarubicin-JGT conjugates. Following three washes in ice-cold RPMI-1640 medium (4 mL/wash), the cells are resuspended in fresh medium and transferred to 96-well plates (100 μL/well). Each tube is set up in duplicate and two wells are plated out per tube (a total of 4 wells per drug concentration). Cells are pulsed with [3H]thymidine 24 hours later and harvested. (Only for Reference) |
| 激酶实验 | CYP450 metabolism experiments: Evaluation of Idarubicin metabolism by the CYP450 isoenzymes 3A4, 2D6, 2C8, 2C9, and 1A2 is completed using isolated human CYP450 proteins for each isoform. The high throughput P450 inhibition testing method is utilized for these evaluations. The metabolism experiments are designed to investigate the following properties of each drug: (1) if Idarubicin is a substrate of the CYP450 3A4, 2C8, 2C9, 1A2 or 2D6 isoenzymes; (2) if metabolism is affected by known inhibitors of each isoenzyme; (3) if Idarubicin is inhibitors of CYP450 isoenzymes; and (4) if caspofungin or itraconazole inhibit the CYP450 metabolism of Idarubicin. Dibenzylfluorescein (DBF) (CYP3A4, CYP2C8, CYP2C9), 3-cyano-7-ethoxycoumarin (Cyp1A2), and 7-methoxy-4-(aminomethyl)-coumarin (MAMC) (CYP2D6) are the known substrates utilized as controls to confirm the respective isoenzyme activity and evaluate the effects of Idarubicin on the isoenzyme activity. In addition, ketoconazole, quercetin, suflaphenazole, furafylline, and quinidine are utilized as control CYP450 inhibitors for 3A4, 2C8, 2C9, 1A2 or 2D6 isoenzymes, respectively. The substrate, inhibitor plus Idarubicin as indicated are added to each protein sample are incubated for 20 minutes- 60 minutes, as recommend by manufacturer, at 37oC. Reactions are stopped with an organic solvent solution and then samples are analyzed by fluorescence plate reader as appropriate. For each experiment, control samples with a known amount of substrate and synthesized metabolite, in the absence of the isoenzyme, are prepared for qualitative comparisons. All experiments are performed in triplicate. |
| 体外活性 | Idarubicin对多细胞球体展现出显著的细胞毒性活性，与其对单层细胞的抗增殖效果相当。[1] Idarubicin还能抑制CYP450 2D6的活性。[2] 与多柔比星和表柔比星相比，Idarubicin的活性分别约为57.5倍和25倍。Idarubicin能够克服P-糖蛋白介导的多药耐药性。[3] Idarubicin能够抑制中性粒细胞超氧化物自由基的形成。[4] Idarubicin可以与单克隆抗体（抗Ly-2.1、抗L3T4或抗Thy-1）耦合，同时保持蛋白质的溶解性和抗体活性。[5] Idarubicin抑制NALM-6细胞的增殖，IC50为12 nM。[6] |
| 体内活性 | Idarubicin的还原依赖于酮还原酶，并且相较于大多数酮类化合物，其还原过程具有更高的立体选择性，几乎专一性地生成(13S)-表构异构体。Idarubicin还原的高立体特异性可能源自于其羰基附近不对称中心的手性诱导效应。[7] |
| 存储条件 | Keep away from direct sunlight,Keep away from moisture,
Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | H2O : 5 mg/mL (9.36 mM), Sonication is recommended.
DMSO : 255 mg/mL (477.57 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.18 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
|
| 关键字 | Topoisomerase | Topo II (MCF-7 cells) | Myc | MCF-7 | leukaemias | Inhibitor | inhibit | Idarubicin Hydrochloride | Idarubicin | Fungal | DNA/RNA Synthesis | DNA synthesis | c-Myc | breast tumor | Bacterial | Autophagy | Antibiotic | 4-Demethoxydaunorubicin Hydrochloride | 4-Demethoxydaunorubicin |
| 相关产品 | Guanidine hydrochloride | Aceglutamide | Calcium Propionate | Neomycin sulfate | Terbinafine hydrochloride | Hemin | Sodium bicarbonate | Hyaluronic acid sodium (MW 20 kDa) | Thymidine | Sodium diacetate | Sulfamethoxazole sodium | D(+)-Raffinose pentahydrate |
| 相关库 | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compound Library | Bioactive Compounds Library Max | Anti-Fungal Compound Library | Failed Clinical Trials Compound Library | Anti-Aging Compound Library | FDA-Approved Drug Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library |
*订购须知：
1.氚试特主营中高端生物试剂耗材，我们的经营理念是"把订试剂变得有意思！"。由于科研商品种类繁多，标定的商品图片仅作参考。工厂或因包材、批次变更等因素更换供货瓶子或其他包装，不影响产品品质，交货标准及瓶子包装以工厂当批次实际供货为准。如需售前确认，可与我们服务团队咨询，我们乐意为您提供优质的服务。
2.广东大部分高校可享受送货至实验室的服务。部分高校、企业可能受配送服务范围、门禁等因素影响，下单前可咨询我司线上服务团队，了解最新配送范围。氚试特/Trust将持续不断的扩充配送范围，为您提供优质的服务。
3.如因天气、大型促销活动等不可抗逆的因素影响，可能影响配送时间，我司配送员会及时与您联系协商配送时间。
4.科研试剂耗材大部分商品因运输等特殊性，非质量问题无法退换货。请下单前确认好产品参数，氚试特/Trust服务团队可提供专业的售前咨询服务。部分品牌非质量问退货换货可能需要您承担退货服务费，请务必确定好再下单。
5.我们深知科研领域对货物及时性的需求，并十分注重科学家的下单体验。一般视品牌每日发货截单时间不同到货时间可能有1天差异。大多品牌每日审批通过后下午15:30前可当日发货，部分品牌为17:00截单。氚试特/Trust每日接收到订单后会第一时间将订单及时送达到工厂仓库，一般当日晚上或次日上午9:30前更新运输单号，请您放心选购。如有十万火急的情况，请与我们服务团队协商。
6.自2025年1月1日起，我们联动科檬商城（科檬/ChemMole），开通订购积分功能。订单金额每满￥50=1积分。订单款项结算后，科檬系统会自动积分。锐竞平台订购的商品会自动同步积分。如您有积分的需求，请联系我们服务团队开通。
7.科檬积分致力于科学家们科研补贴补助，仅限用于科研或与科研建设相关用途，未经学校允许不得用于个人用途。
8.针对年订购量达10万以上或批量集采的课题组单位，可与我们开通VIP增值服务通道，我们将在打包选品及配送上为您提供个性化方案。
9.其他未尽事宜，欢迎随时与我们沟通。氚试特/Trust祝您在研途上一往无前，乘风破浪！
正品保障
授权代理 严苛选品
品种齐全
专业供应链 百万货源
合规保障
合规资质 售后无忧
