Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ONC206 是一种 ONC201 的类似物,是一种多巴胺 D2- 样受体 (DRD2/3/4) 的选择性拮抗剂,其拮抗作用在纳摩尔级别。它具有广谱抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 372 | 现货 | ||
2 mg | ¥ 518 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 1,370 | 现货 | ||
25 mg | ¥ 2,680 | 现货 | ||
50 mg | ¥ 3,950 | 现货 | ||
100 mg | ¥ 5,620 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 885 | 现货 |
产品描述 | ONC206, an analogue of the TRAIL inducer ONC201, acts as a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations and possesses broad-spectrum anti-tumor activity. |
体外活性 | ONC206 (Oncoceutics) is an imipiridone with nanomolar potency and analogue of ONC201, a selective dopamine receptor D2 (DRD2) antagonist currently being investigated in phase II clinical trials for serous endometrial cancer (SEC).??ONC206 inhibited cellular proliferation in a dose-dependent manner and was more potent than ONC201 in the ARK1 (IC50 = 0.33 M vs. IC50 = 1.59uM) and SPEC-2 (IC50 = 0.24uM vs. IC50 = 0.81uM) cell lines.?Treatment with ONC206 resulted in induction of ROS production and reduction of mitochondrial membrane potential, accompanied by an increase in cleaved caspase-3 and caspase-9 activity (p 0.01).?ONC206 also significantly inhibited cellular adhesion and migration in both cell lines (p 0.01).?Pretreatment with the stress inhibitor N-acetylcysteine (NAC) significantly attenuated the efficacy of ONC206 on cell proliferation, ROS production and cellular invasion.?ONC206 demonstrates nanomolar potency for the inhibition of proliferation in SEC cells[3]. |
体内活性 | ONC206 (100 mg/kg; p.o.; every 10 days) reduces obviously tumor growth inhibition[2]. |
分子量 | 408.44 |
分子式 | C23H22F2N4O |
CAS No. | 1638178-87-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (244.83 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 | 2.4483 mL | 12.2417 mL | 24.4834 mL | 61.2085 mL |
5 mM | 0.4897 mL | 2.4483 mL | 4.8967 mL | 12.2417 mL | |
10 mM | 0.2448 mL | 1.2242 mL | 2.4483 mL | 6.1209 mL | |
20 mM | 0.1224 mL | 0.6121 mL | 1.2242 mL | 3.0604 mL | |
50 mM | 0.049 mL | 0.2448 mL | 0.4897 mL | 1.2242 mL | |
100 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6121 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。
ONC206 1638178-87-6 GPCR/G Protein Neuroscience Dopamine Receptor antagonist Inhibitor ONC201 DRD2/3/4 inhibit receptors D2-like ONC 206 dopamine ONC-206 inhibitor