Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2879552 2HCl (1401966-69-5(free base)) 是一种口服的、不可逆的赖氨酸特异性去甲基化酶 1 (LSD1) 抑制剂,具有潜在的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 530 | 现货 | ||
2 mg | ¥ 760 | 现货 | ||
5 mg | ¥ 1,080 | 现货 | ||
10 mg | ¥ 1,800 | 现货 | ||
25 mg | ¥ 2,990 | 现货 | ||
50 mg | ¥ 4,200 | 现货 | ||
100 mg | ¥ 5,990 | 现货 | ||
500 mg | ¥ 12,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,080 | 现货 |
产品描述 | GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. |
靶点活性 | LSD1: |
体外活性 | GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1]. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min?1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM |
体内活性 | GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice |
细胞实验 | Viable cells are measured in Cell Counting Kit-8 (CCK8) assay. Briefly, cells are cultured in a 96-well plate overnight at a density of 5×103 cells per well and treated with the indicated concentrations of sorafenib (0 μM, 40 μM or 80 μM) for 24 h. Subsequently, the cells are incubated with 10 μL CCK8 for 60 min at 37°C, 5% CO2. The absorbance of optical density at 450 nm (A450) is determined with Varioskan Flash. |
分子量 | 437.41 |
分子式 | C23H30Cl2N2O2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.37 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2862 mL | 11.4309 mL | 22.8618 mL | 57.1546 mL |
5 mM | 0.4572 mL | 2.2862 mL | 4.5724 mL | 11.4309 mL | |
10 mM | 0.2286 mL | 1.1431 mL | 2.2862 mL | 5.7155 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。
GSK2879552 2HCl (1401966-69-5(free base)) Chromatin/Epigenetic Histone Demethylase GSK2879552 2HCl (1401966 69 5(free base)) GSK2879552 2HCl (1401966695(free base)) GSK-2879552 2HCl (1401966-69-5(free base)) Inhibitor inhibitor inhibit