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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-ONC206
ONC206

Chemical Structure : ONC206

CAS No.: 1638178-87-6

ONC206 (ONC-206, ONC 206)

货号: PC-72174Not For Human Use, Lab Use Only.

ONC206 (ONC 206) is a chemical analogue of ONC201, a selective antagonist of dopamine D2-like receptor (DRD2, Ki=320 nM) with broad-spectrum anti-tumor activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ONC206 (ONC 206) is a chemical analogue of ONC201, a selective antagonist of dopamine D2-like receptor (DRD2, Ki=320 nM) with broad-spectrum anti-tumor activity.
ONC206 does not inhibit the D1-like (DRD 1/5), subfamily of dopamine receptors.
ONC206 has highly potent activity in preclinical models of difficult-to-treat neuroendocrine tumors and sarcomas.
ONC206 possesses a ~10-fold increased affinity for DRD2 compared to ONC201 with a Ki of ~320nM with selectivity that was superior to approved antipsychotics.
ONC206 is highly efficacious in neuroblastoma (GI50 87-589nM) including cell lines derived from metastatic sites and with MYCN amplification associated with poor prognosis.
ONC206 (100 mg/kg PO every 10 days) causes significant tumor growth inhibition in MHH-ES-1 athymic nude mice xenografts.

物理化学性质&存储条件

分子量 408.453
分子式 C23H22F2N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-benzyl-4-(2,4-difluorobenzyl)-2,4,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one

参考文献

1. Wagner J, et al. Cell Cycle. 2017 Oct 2;16(19):1790-1799.

2. Hu W, et al. Cancers (Basel). 2020 Aug 27;12(9):2436.

3. Staley A, et al. Am J Cancer Res. 2021 Nov 15;11(11):5374-5387.

4. Varun Vijay Prabhu, et al. Cancer Res 2017;77.

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