Powder: -20°C for 3 years | In solvent: -80°C for 1 year
K-756 是一种直接的 tankyrase(TNKS) 选择性抑制剂,对 TNKS1和 TNKS2的 ADP-核糖基化活性有抑制作用,IC50分别为 31 和 36 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 456 | 现货 | ||
5 mg | ¥ 995 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,460 | 现货 | ||
50 mg | ¥ 4,970 | 现货 | ||
100 mg | ¥ 7,230 | 现货 | ||
500 mg | ¥ 14,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,170 | 现货 |
产品描述 | K-756 is a direct and selective inhibitor of tankyrase (TNKS), which inhibits the ADP-ribosylation activity of TNKS1 (IC50 = 31 nM) and TNKS2 (IC50 = 36 nM). |
靶点活性 | TNKS1:31 nM, TNKS2:36 nM |
体外活性 | K-756 inhibits the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. K-756 is a novel and selective Wnt/β-catenin pathway inhibitor targeting tankyrase (TNKS). TNKS is one of the members of the PARP family. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. K-756 inhibits TNKS1 and TNKS2 by 97% and 100%, respectively. The inhibitory activity of K-756 against PARP1, PARP2, PARP3, PARP6, PARP7, and PARP11 is less than 13%. K-756 strongly inhibits the reporter activity in DLD-1/TCF-Luc cells (IC50: 110 nM) but does not inhibit DLD-1/mtTCF-Luc cells, even at 1,000 nM. APC-mutant colorectal cancer cell line COLO 320DM and SW403 cells are treated with K-756 and after 144 hours, cell growth inhibition is measured by an XTT assay. The application of K-756 inhibits the cell growth of COLO 320DM with a GI50 of 780 nM. K-756 also inhibits SW403 with a GI50 of 270 nM[1]. |
体内活性 | Vehicle (0.5% MC400) or K-756 is administered orally once a day for 3 days at 100, 200, and 400 mg/kg. The Wnt/β-catenin signal inhibition in the tumor is detected by measuring FGF20 and LGR5 and luciferase activity. The Wnt/β-catenin signal inhibition at a dose of 400 mg/kg is observed from 1-day administration. The expression of FGF20 and reporter activity are significantly decreased at doses of 100 mg/kg and above at 3-day administration. The expression of LGR5 is significantly decreased at doses of 200 mg/kg and above at 3-day administration. The maximum inhibitory activity is reached with the administration of K-756 at a dose of 400 mg/kg at 3-day administration [1]. |
分子量 | 433.5 |
分子式 | C24H27N5O3 |
CAS No. | 130017-40-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.5 mg/mL (10.38 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3068 mL | 11.534 mL | 23.0681 mL | 57.6701 mL |
5 mM | 0.4614 mL | 2.3068 mL | 4.6136 mL | 11.534 mL | |
10 mM | 0.2307 mL | 1.1534 mL | 2.3068 mL | 5.767 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。
K-756 130017-40-2 Chromatin/Epigenetic Cytoskeletal Signaling DNA Damage/DNA Repair Stem Cells PARP Wnt/beta-catenin Inhibitor poly ADP ribose polymerase K756 K 756 inhibit inhibitor