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ONC206 {[allProObj[0].p_purity_real_show]}

货号:A1155605

ONC206 是 ONC201 的类似物。ONC206 是一种选择性拮抗剂,对多巴胺 D2 类受体 (DRD2/3/4) 具有纳摩尔效力。ONC206 表现出广谱抗肿瘤活性。

ONC206 化学结构 CAS号:1638178-87-6
ONC206 化学结构
CAS号:1638178-87-6
ONC206 3D分子结构
CAS号:1638178-87-6
ONC206 化学结构 CAS号:1638178-87-6
ONC206 3D分子结构 CAS号:1638178-87-6
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ONC206 纯度/质量文件 产品仅供科研

货号:A1155605 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

+++

D4 receptor (human), Ki: 7.5 nM

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
Clozapine N-oxide 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ONC206 生物活性

靶点
  • D2 receptor

描述 ONC206 is a derivative of the TRAIL inducer ONC201[1]. ONC206 selectively antagonizes D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 exhibits wide-ranging antitumor efficacy[2].
体内研究

ONC206 (100 mg/kg;pO.; every 10 days) results in notable inhibition of tumor growth[2].

体外研究

ONC206 exhibits selective antagonism towards the D2-like (DRD2/3/4), rather than the D1-like (DRD1/5), subfamily of dopamine receptors[2].

ONC206 markedly suppresses tumor cell migration and invasion in vitro[1].

ONC206 (0.05 μM; for 48 hours) impedes the migration of ONC201- and TRAIL-resistant HCT116 Bax cells without eliciting cell death or hindering cell proliferation[1].

ONC206 activates the ISR and TRAIL pathway, resulting in tumor growth arrest and cell death[1].

ONC206 does not cause cell cycle arrest in a colorectal cell line that has developed resistance to ONC201[1].

ONC206 参考文献

[1]Wagner J, et al. Preclinical evaluation of the imipridone family, analogs of clinical stage anti-cancer small molecule ONC201, reveals potent anti-cancer effects of ONC212. Cell Cycle. 2017 Oct 2;16(19):1790-1799.

[2]Varun Vijay Prabhu, et al. Potent anti-cancer activity of the imipridone ONC206: A selective dopamine D2-like receptor antagonist. AACR Annual Meeting 2017, April 1-5, 2017; Washington, DC.

ONC206 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.24mL

12.24mL

2.45mL

1.22mL

24.48mL

4.90mL

2.45mL

ONC206 技术信息

CAS号1638178-87-6
分子式C23H22F2N4O
分子量 408.444
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(122.42 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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