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Tosedostat

Tosedostat

产品编号 T6301   CAS 238750-77-1
别名: CHR-2797, 托舍多特

Tosedostat (CHR-2797) 是一种具有口服活性的氨基肽酶(aminopeptidase) 抑制剂,对多种肿瘤细胞系均具有抗增殖作用。

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Tosedostat Chemical Structure
Tosedostat, CAS 238750-77-1
规格 价格/CNY 货期 数量
1 mg ¥ 472 现货
2 mg ¥ 737 现货
5 mg ¥ 1,490 现货
10 mg ¥ 2,280 现货
25 mg ¥ 3,380 现货
50 mg ¥ 4,820 现货
100 mg ¥ 6,690 现货
1 mL * 10 mM (in DMSO) ¥ 1,590 现货
产品目录号及名称: Tosedostat (T6301)
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纯度: 99.4%
纯度: 98.86%
纯度: 98.14%
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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 Tosedostat (CHR-2797) is an orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death.
体外活性 In HL-60 cells, the treatmentwith Tosedostat (CHR-2797) results in an increase in the secretion of Stanniocalcin 2 (STC2) protein into the growth medium. After 2 h treatment with Tosedostat (60 nM), increases in SLC7A11 expression are detectable. The for by Tosedostat inhibits the proliferation of U-937 and HuT 78 cell lines (IC50s: 10 nM; >10 μM). Tosedostat treatment increases expression of amino acid deprivation response (AADR) genes in U-937 cells but not in HuT 78 cells. By 24 h with Tosedostat (0.01 μM) the mean MCA production is reduced to 77.8% of the untreated control cells; similarly the MCA production is reduced to 51.3% with 1 μM, 38.5% with 5 μM, and 35.3% with 10 μM Tosedostat.
体内活性 In vivo in rodent cancer models, Tosedostat (CHR-2797) has anticancer activity, and a dose-response relationship has been shown in two models. The effect of Tosedostat is less apparent when the tumor burden is higher before therapy.
激酶实验 Cells are seeded at a density of 4×104/mL, cultured for 24 h, then treated with 0.06 to 6 μM Tosedostat (CHR-2797) for 24 h. After treatment, 5×104 cells are washed with PBS and seeded in 100 μL Cys/Met-free RPMI 1640 containing Tosedostat, supplemented with 10% dialyzed FBS. 1.5 μCi [35S]Cys/Met (>1,000 Ci/mmol) is added, and incubation continued for 1 h at 37°C. Cells are captured onto 96-well GF/B filter plates and washed twice with PBS before precipitation with 10% ice-cold trichloroacetic acid (TCA) for 1 h at 4°C. Precipitated proteins are washed four times with ice-cold 10% TCA and air-dried for 1 h. UltimaGold scintillation cocktail is added and allowed to mix for 1 h before scintillation counting using a scintillation counter.
细胞实验 Tosedostat (CHR-2797) is stored at -20°C as a 10 mM stock in dimethyl sulfoxide (DMSO), and diluted with RPMI culture medium prior to use.Leukemic cells are washed and suspended in phosphate buffered saline (PBS). 100 μL of cell suspension (1×105 cells/mL) is mixed with 100 μL of Tosedostat (CHR-2797) (0.01 to 10 μM) and 200 μM L-alanine 4-methyl-coumaryl-7-amide (ala-MCA) in a 96 well plate in duplicate. The aminopeptidase activity is measured by detecting the fluorescent 7-amino-4-methylcoumarin (MCA) liberated from the cleavage of ala-MCA by cellular aminopeptidases (excitation 355 nm, emission 460 nm).
动物实验 A breeding colony of NOD/SCID IL2R gammanull mice are used in this study. The mice are inoculated subcutaneously in the right flank with 2×106 H929 myeloma cells in 50 μL RPMI-1640 and 50 μL MatrigelTM Basement Membrane Matrix Growth Factor Reduced. The mice are assigned into the following four treatment groups (10 animals per group): no treatment, Tosedostat 75 mg/kg, CHR-3996 30 mg/kg, and Tosedostat 75 mg/kg with concomitant CHR-3996 30 mg/kg. Tosedostat is administered daily by intra-peritoneal injection beginning four days after the tumour cells are inoculated. Caliper measurements of the longest perpendicular tumour diameters (length) and width are performed every other day to estimate the tumour volume.
别名 CHR-2797, 托舍多特
分子量 406.47
分子式 C21H30N2O6
CAS No. 238750-77-1

存储

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

溶解度

DMSO: 55 mg/mL (135.31 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4602 mL 12.301 mL 24.6021 mL 61.5052 mL
5 mM 0.492 mL 2.4602 mL 4.9204 mL 12.301 mL
10 mM 0.246 mL 1.2301 mL 2.4602 mL 6.1505 mL
20 mM 0.123 mL 0.6151 mL 1.2301 mL 3.0753 mL
50 mM 0.0492 mL 0.246 mL 0.492 mL 1.2301 mL
100 mM 0.0246 mL 0.123 mL 0.246 mL 0.6151 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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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. van Herpen CM, et al. Br J Cancer. 2010 Oct 26;103(9):1362-8. 2. Jenkins C, et al. Leuk Res. 2011 May;35(5):677-81. 3. Krige D,etal.CHR-2797: an antiproliferative aminopeptidase inhibitor that leads to amino acid deprivation in human leukemic cells.Cancer Res. 2008 Aug 15;68(16):6669-79. 4. Smith EM, et al.The combination of HDAC and aminopeptidase inhibitors is highly synergistic in myeloma and leads to disruption of the NFκB signalling pathway.Oncotarget. 2015 Jul 10;6(19):17314-27.
L-Hyoscyamine YM-46303 Ethidium bromide DMAB-anabaseine dihydrochloride Atractyloside A (Rac)-ABT-202 dihydrochloride Pentolinium Tartrate nAChR agonist 1

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌上市药物库 抗癌活性化合物库 ReFRAME 相关化合物库 口服活性化合物库 药物功能重定位化合物库 神经信号分子库 上市药物库 FDA上市及药典收录分子库

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
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% 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

Tosedostat 238750-77-1 Metabolism Neuroscience AChR Aminopeptidase CHR-2797 托舍多特 CHR2797 CHR 2797 inhibit Inhibitor inhibitor

 

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