化合物ONC206 T16392

Product Introduction
Bioactivity


英文名: ONC206

描述: 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。

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
体内活性: ONC206（100 mg/kg；口服；每10天一次）明显减缓了肿瘤生长[2]。

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

溶解度: DMSO : 100 mg/mL (244.83 mM)


关键字: antagonist | Inhibitor | ONC201 | DRD2/3/4 | inhibit | receptors | ONC206 | D2-like | Dopamine Receptor | ONC 206 | dopamine | ONC-206

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途