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Exatecan Mesylate

产品编号 TQ0088 CAS 169869-90-3

别名: 依沙替康甲磺酸盐, 依喜替康甲磺酸盐, DX8951f

Exatecan Mesylate (DX8951f) 是一种 DNA 拓扑异构酶 I 抑制剂，IC50值为 2.2 μM，可研究癌症。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Exatecan Mesylate Chemical Structure

Exatecan Mesylate, CAS 169869-90-3

规格	价格/CNY		货期	数量
5 mg	￥ 177		现货

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其他形式的 Exatecan Mesylate:

Exatecan
现货

选择批次

纯度: 99.89%

纯度: 99.89%

纯度: 99.44%

纯度: 97.32%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).
靶点活性	Topo I:2.2 μM
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]。
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].
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].
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].

别名	依沙替康甲磺酸盐, 依喜替康甲磺酸盐, DX8951f
分子量	531.55
分子式	C25H26FN3O7S
CAS No.	169869-90-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 8 mg/mL (15.05 mM), Sonification is recommended.

H2O: 6 mg/mL (11.29 mM), Sonification and heating are recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	1.8813 mL	9.4065 mL	18.8129 mL	47.0323 mL
	5 mM	0.3763 mL	1.8813 mL	3.7626 mL	9.4065 mL
	10 mM	0.1881 mL	0.9406 mL	1.8813 mL	4.7032 mL

计算器

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参考文献

1. Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82. 2. Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7;72(4):680-6. 3. Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1;63(1):80-5.

相关产品

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Moxifloxacin hydrochloride CPT-Se3 Levofloxacin SN-38 Exatecan TAS-103 dihydrochloride AuM1Phe CPT-Se4

相关化合物库

该产品包含在如下化合物库中：

抑制剂库抗癌临床化合物库药物功能重定位化合物库抗癌活性化合物库抗癌药物库抗癌化合物库临床期小分子药物库儿童药物库抗卵巢癌化合物库抗肺癌化合物库

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

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每只动物体重

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给药体积

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动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Exatecan Mesylate 169869-90-3 DNA Damage/DNA Repair Topoisomerase Exatecan 依沙替康甲磺酸盐依喜替康甲磺酸盐 Inhibitor inhibit DX8951f inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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