ONC206

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ONC206 是 TRAIL 诱导剂 ONC201 的类似物，是纳摩尔浓度的 D2 样多巴胺受体 (DRD2/3/4) 的选择性拮抗剂。 ONC206 还具有广谱抗肿瘤活性。 ONC206 (Oncoceutics) 是一种具有纳摩尔效力的咪啶酮，是 ONC201 的类似物，ONC201 是一种选择性多巴胺受体 D2 (DRD2) 拮抗剂，目前正在进行浆液性子宫内膜癌 (SEC) 的 II 期临床试验。

ONC206 is an analogue of TRAIL inducer ONC201 and is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 also has broad-spectrum anti-tumor activity. 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

Cell Proliferation Assay Cell Line:HCT116 cells Concentration:0.05 μM Incubation Time:Over 48 hours Result:Inhibited migration of ONC201- and TRAIL-resistant HCT116 Bax?/? cells.

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GPCR/G Protein

Dopamine Receptor

Dopamine

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1638178-87-6

408.44

C23H22F2N4O

>98% (HPLC)

DMSO:100 mg/mL (244.83 mM; Need ultrasonic)

FC1=CC(F)=CC=C1CN2C(C(C3)=C(N4CCN=C42)CCN3CC5=CC=CC=C5)=O

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(-20℃)

With Ice Pack

≥ 2 years