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Tasisulam

Tasisulam

产品编号 T6191   CAS 519055-62-0
别名: LY573636, 他司磺胺

Tasisulam (LY573636) 是一种小分子抗肿瘤药物,通过内在途径诱导细胞凋亡,导致细胞色素 c 释放和 caspase 依赖性细胞死亡。它抑制有丝分裂进程并诱导血管正常化。

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Tasisulam Chemical Structure
Tasisulam, CAS 519055-62-0
规格 价格/CNY 货期 数量
1 mg ¥ 149 现货
5 mg ¥ 332 现货
10 mg ¥ 533 现货
25 mg ¥ 1,190 现货
50 mg ¥ 1,980 现货
100 mg ¥ 2,960 现货
200 mg ¥ 4,360 现货
500 mg ¥ 6,780 现货
1 mL * 10 mM (in DMSO) ¥ 516 现货
其他形式的 Tasisulam:
产品目录号及名称: Tasisulam (T6191)
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选择批次  
纯度: 99.97%
纯度: 99.77%
纯度: 99%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tasisulam (LY573636) is an apoptosis inducer and an antitumor agent via the intrinsic pathway.
体外活性 Tasisulam inhibits growth of various human leukemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. LY573636 also induces apoptosis in HL60, Reh, and MD901 cells, mainly by loss of mitochondrial membrane potential and induction of reactive oxygen species. [1] In addition, Tasisulam also produce antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. Tasisulam induces G2–M accumulation and subsequent apoptosis in Calu-6 and A-375 cells. In vitro, Tasisulam also inhibits VEGF-, FGF- and EGF-induced endothelial cord formation with EC50 of 47, 103, and 34 nM, respectively. [2]
体内活性 Tasisulam induces morphologic features of vascular normalization, including increased pericyte coverage and decreased hypoxia in vivo. Tasisulam (25 or 50 mg/kg, i.v.) displays dose-dependent antitumor activity, induces apoptosis, and normalizes tumor-associated vasculature in the Calu-6 non–small cell lung xenograft model. Besides, Tasisulam displays potent antitumor activity across a range of in vivo xenografts, including colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukemia (MV-4-11), and pancreatic (QGP-1). [2]
激酶实验 Electrophysiology: The human IKCa1 is cloned and expressed in COS-7 cells. Cells are studied in the whole-cell configuration of the patch-clamp technique. The holding potential is 280 mV. The internal pipette solution contains: 145 mM K+ aspartate, 2 mM MgCl2, 10 mM Hepes, 10 mM K2EGTA, and 8.5 mM CaCl2 (1 μM free Ca2+), pH 7.2, 290-310 mOsm. To reduce currents from the native chloride channels in COS-7 cells, Na+ aspartate Ringer is used as an external solution: 160 mM Na+ aspartatey/4.5 mM KCl/2 mM CaCl2/1 mM MgCl2/5 mM Hepes, pH 7.4/290-310 mOsm. IKCa currents in COS-7 cells are elicited by 200-ms voltage ramps from -120 mV to 40 mV applied every 10 seconds and the reduction of slope conductance at -80 mV by TRAM-34 taken as a measure of channel block.
细胞实验 Cells are treated with various concentrations of LY573636. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay is performed. Briefly, MTT is dissolved in phosphate-buffered saline (PBS) at 5 mg/mL. Approximately 1,000 cells per well are incubated in culture medium for 96 hours in 96-well plates; and then, 10 μL of the MTT solution is added. After a 4-hour incubation, 100 μL of solubilization solution (20 % sodium dodecyl sulfate [SDS]) is added, and the mixture was incubated at 37 °C for 16 hours. In this assay, MTT is cleaved to an orange formazan dye by metabolically active cells; and the absorbance of the formazan product is measured with an enzyme-linked immunoabsorbent assay (ELISA) reader at 540 nm. (Only for Reference)
别名 LY573636, 他司磺胺
分子量 415.11
分子式 C11H6BrCl2NO3S2
CAS No. 519055-62-0

存储

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

溶解度

Ethanol: 77 mg/mL (185.5 mM)

DMSO: 77 mg/mL (185.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.409 mL 12.045 mL 24.09 mL 60.225 mL
5 mM 0.4818 mL 2.409 mL 4.818 mL 12.045 mL
10 mM 0.2409 mL 1.2045 mL 2.409 mL 6.0225 mL
20 mM 0.1205 mL 0.6023 mL 1.2045 mL 3.0113 mL
50 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2045 mL
100 mM 0.0241 mL 0.1205 mL 0.2409 mL 0.6023 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Haritunians T, et al. Oncol Rep. 2008, 20(5), 1237-1242. 2. Meier T, et al. Mol Cancer Ther. 2011, 10(11), 2168-2178.
Panobinostat OSU-T315 Epothilone B Tandutinib SPOP-IN-6lc Gemcitabine elaidate Etalocib Tomatine

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 NO PAINS 化合物库 细胞焦亡化合物库 抗癌化合物库 抗肺癌化合物库 临床前化合物库 细胞凋亡化合物库 药物功能重定位化合物库

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
mg/kg
每只动物体重
g
给药体积
μL
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
%
% Tween 80
% ddH2O
计算 重置

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

Tasisulam 519055-62-0 Apoptosis Proteases/Proteasome Caspase LY 573636 LY-573636 inhibit Inhibitor LY573636 他司磺胺 inhibitor

 

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