Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK-3685032 是一种非时间依赖、非共价、选择性的、可逆的DNMT1抑制剂,IC50=0.036 μM。它诱导 DNA 甲基化丧失、转录激活和癌细胞生长抑制。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 658 | 现货 | ||
5 mg | ¥ 1,580 | 现货 | ||
10 mg | ¥ 2,390 | 现货 | ||
25 mg | ¥ 4,590 | 现货 | ||
50 mg | ¥ 6,570 | 现货 | ||
100 mg | ¥ 8,860 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,730 | 现货 |
产品描述 | GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth. |
靶点活性 | DNMT1:36 nM |
体外活性 | In MV4-11 cells, GSK3685032 (0.1-1000 nM, 1-6 days) exhibited growth inhibition after 3 days, with decreasing growth IC50 throughout a 6 d time course. GSK3685032 (10-10000 nM, day 4) increased the immune-related gene transcription in a dose dependent manner[1]. GSK3685032 (3.2-10,000 nM, 2 days) inhibited DNMT1 protein expression. In 15 leukemia, 29 lymphoma and 7 multiple myeloma cell lines, e.g., EOL-1, Ki-JK, MM.IR cells, GSK3685032 (6 days) showed cell growth inhibition of majority cancer cell lines, with a median growth IC50 value of 0.64 μM. GSK3685032 induced DNA hypomethylation and gene activation[1]. |
体内活性 | In MV4-11 xenograft models or SKM-1 xenograft models, GSK-3685032 (1-45 mg/kg; s.c.) inhibited dose-dependent tumor growth with clear regression at ≥30 mg/kg[1]. |
分子量 | 420.53 |
分子式 | C22H24N6OS |
CAS No. | 2170137-61-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (23.78 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.378 mL | 11.8898 mL | 23.7795 mL | 59.4488 mL |
5 mM | 0.4756 mL | 2.378 mL | 4.7559 mL | 11.8898 mL | |
10 mM | 0.2378 mL | 1.189 mL | 2.378 mL | 5.9449 mL | |
20 mM | 0.1189 mL | 0.5945 mL | 1.189 mL | 2.9724 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。
GSK3685032 2170137-61-6 Chromatin/Epigenetic DNA Methyltransferase Inhibitor lymphoma DNMTs cancer DNA MTases inhibit GSK-3685032 GSK 3685032 MV4–11 leukemia GDM-1 multiple myeloma inhibitor