Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 77 mg/mL (185.5 mM)
DMSO: 77 mg/mL (185.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Tasisulam 519055-62-0 Apoptosis Proteases/Proteasome Caspase LY 573636 LY-573636 inhibit Inhibitor LY573636 他司磺胺 inhibitor