基本信息 产品详情 公司简介 推荐产品
  • 首页
  • 个人中心
  • 委托采购
  • 采购清单
网站主页 化工产品目录 生物 生物化学试剂 拮抗剂 甲磺酸伊喜替康 依喜替康甲磺酸盐
  • 依喜替康甲磺酸盐|TQ0088

依喜替康甲磺酸盐|TQ0088

Exatecan Mesylate
169869-90-3
￥177.00 5瓶 起订
上海 更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
依喜替康甲磺酸盐
英文名称：
Exatecan Mesylate
CAS号：
169869-90-3
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.
纯度规格：
99.89%
产品类别：
抑制剂
货号：
TQ0088

Product Introduction

Bioactivity

名称Exatecan Mesylate
描述Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).
细胞实验Growth inhibition experiments are carried out in 96-well flat-bottomed microplates, and the amount of viable cells at the end of the incubation is determined by MTT assay. Thus, 500-20000 cells/well in 150 μL of medium are plated and grown for 24 h (P388, CCRF-CEM and K562 cells for 4h), the drug (including Exatecan Mesylate, in 150 μL medium/well), or the medium alone as a control, is added, and the cells are cultured for an additional 3 days. After the addition of MTT (20 μL/well, 5 mg/mL in phosphate-buffered saline), the plates are incubated for 4 h and centrifuged at 800 g for 5 min, then the medium is removed and the blue dye formed is dissolved in 150 μL of DMSO. the absorbance is measured at 540 nm using a Microplate Reader [1].
激酶实验Cells (5×10^6) are lysed with SDS buffer (10 mM HEPES, 2 mM orthovanadate, 10 mM NaF, 10 mM pyrophosphate, 1 mM PMSF, 10 μg/mL leupeptin, 10% 2-mercaptoethanol, 10% glycerol,8% SDS, 42 mM Tris-HCl, 0.002% bromophenol blue, pH 7.4). Protein in the whole-cell lysates is separated in 7.5% polyacrylamide gel and blotted onto the nitrocellulose membrane. The membrane is treated with anti-Topo I human antibody and subsequently, with horseradish peroxidase-conjugated protein A. The Topo I-specific band is detected with ECL reagents. To obtain a nuclear extract, cells (5×10^7) are washed with ice-cold buffer (2 mM K2HPO4, 5 mM MgCl2, 150 mM NaCl, 1 mM EGTA, 0.1 mM dithiothreitol), resuspended in buffer containing 0.35% Triton-X100 and PMSF and then incubated on ice for 10 min. The resulting lysates are centrifuged, and precipitates are then incubated with buffer containing 0.35 M NaCl for 1 hr at 4°C. After centrifugation (18,000g, 10 min), the protein concentration of the supernatant (nuclear extract) is determined using a protein assay kit. The same amount of nuclear protein is analyzed by Western blotting analysis using the anti-Topo I antibody [2].
动物实验At 3 weeks after BxPC-3-GFP and MIA-PaCa-2-GFP orthotopic implantation, mice are randomized into five different groups of 5 mice each for treatment purposes. Group 1 serves as the negative control and does not receive any treatment. Groups 2 and 3 are treated with Exatecan Mesylate at 25 and 15 mg/kg/dose, respectively. Groups 4 and 5 receive gemcitabine treatments at 300 and 150 mg/kg/dose, respectively. At 6 weeks after BxPC-3-GFP orthotopic implantation, mice are randomized into three different groups of 20 mice each for treatment purposes. Group 1 serves as the negative control and does not receive any treatment. Group 2 is treated with 25 mg/kg/dose Exatecan Mesylate and group 3 receives 300 mg/kg/dose gemcitabine. Dosing for both drugs is performed once a week for 3 weeks, discontinued for 2 weeks, and then continued for another 3 weeks. In both early and late cancer models, primary tumor size and body weights are measured once a week. Tumor volumes are calculated using the formula a × b2 × 0.5, where a and b represent the larger and smaller diameters, respectively. At the termination of the studies, mice are sacrificed and explored. Final tumor weights and direct GFP images of primary tumor and metastases are recorded for each mouse. The tumor growth IR is calculated using the formula IR (%) = (1 ? TWt/TWc) × 100, where TWt and TWc are the mean tumor weight of treated and control groups, respectively [3].
体外活性Exatecan Mesylate (DX-8951f) 显著抑制多种癌症细胞系的增殖，对乳腺癌细胞、结肠癌细胞、胃癌细胞和肺癌细胞的平均GI50分别为2.02 ng/mL、2.92 ng/mL、1.53 ng/mL和0.877 ng/mL [1]。Exatecan 对PC-6和PC-6/SN2-5细胞展示出细胞毒性活动，其平均GI50分别为0.186 ng/mL和0.395 ng/mL。此外，Exatecan Mesylate (34 nM) 在PC-6和PC-6/SN2-5细胞中稳定DNA-TopoI复合体 [2]。
体内活性Exatecan Mesylate（3.325-50 mg/kg，静脉注射）在携带肿瘤细胞的小鼠模型中展示出抗肿瘤活性，未观察到毒性死亡[1]。Exatecan Mesylate（15, 25 mg/kg，静脉注射）在MIA-PaCa-2早期模型及BxPC-3早期模型中，显著抑制MIA-PaCa和BxPC-3原发肿瘤生长。在BxPC-3晚期癌症模型中，Exatecan Mesylate（15, 25 mg/kg，静脉注射）还显著抑制了BxPC-3的淋巴转移，并完全消除了肺转移[3]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 8 mg/mL (15.05 mM), Sonication is recommended.
H2O : 6 mg/mL (11.29 mM), Sonication and heating are recommended.
关键字Exatecan | Exatecan Mesylate | Topoisomerase | Inhibitor | inhibit
相关产品Prulifloxacin | Norfloxacin | Ciprofloxacin | Berberine chloride | Etoposide | Dexamethasone acetate | Ciprofloxacin monohydrochloride | EIDD-1931 | Paclitaxel | Methotrexate
相关库抑制剂库 | 抗乳腺癌化合物库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 抗衰老化合物库 | 抗卵巢癌化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
依喜替康甲磺酸盐|||依沙替康甲磺酸盐|||DX8951f

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 (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

依喜替康甲磺酸盐相关厂家报价 更多

内容声明
official 进入官方账号
拨打电话 立即询价