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  • 盐酸伊达比星|T6010

盐酸伊达比星|T6010

Idarubicin hydrochloride
57852-57-0
167 1mg 起订
426 5mg 起订
683 10mg 起订
上海 更新日期:2026-01-06

TargetMol中国(陶术生物)

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邮箱:marketing@targetmol.com

产品详情:

中文名称:
盐酸伊达比星
英文名称:
Idarubicin hydrochloride
CAS号:
57852-57-0
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别:
抑制剂
货号:
T6010

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Powder: -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 Hydrochloride | Idarubicin | Fungal | DNA/RNA Synthesis | DNA synthesis | c-Myc | breast tumor | Bacterial | Autophagy | Antibiotic | 4-Demethoxydaunorubicin Hydrochloride | 4-Demethoxydaunorubicin
相关产品Aceglutamide | Calcium Propionate | Benzyl propionate | Levulinic acid | Neomycin sulfate | BES | Terbinafine hydrochloride | Dimethyl sulfoxide | Thymidine | Sodium diacetate | Sulfamethoxazole sodium | D(+)-Raffinose pentahydrate
相关库抑制剂库 | 抗癌上市药物库 | 经典已知活性库 | 抗癌活性化合物库 | 抗真菌库 | 已知活性化合物库 | 临床失败化合物库 | 抗衰老化合物库 | FDA 上市药物库 | 抗病毒库 | 药物功能重定位化合物库 | 抗癌药物库
伊达比星盐酸盐|||盐酸伊达比星|||Zavedos|||Idarubicin HCl|||Idamycin|||4-Demethoxydaunorubicin hydrochloride|||4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl|TargetMol

公司简介

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 (13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

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