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首页-小分子抑制剂&激动剂-Apoptosis-TRAIL-ONC201
ONC201

Chemical Structure : ONC201

CAS No.: 41276-02-2

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ONC201 (Dordaviprone, TIC10, ONC-201)

货号: PC-61649Not For Human Use, Lab Use Only.

ONC201 (Dordaviprone, TIC10, ONC-201) is a potent, orally active, and brain-permeable small molecule that transcriptionally induces TRAIL in a p53-independent manner, is a potent caseinolytic protease P (ClpP) activator with EC50 of 1.25 uM.

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10 mg ￥1280 In stock
25 mg ￥1980 In stock
50 mg ￥3280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ONC201 (Dordaviprone, TIC10, ONC-201) is a potent, orally active, and brain-permeable small molecule that transcriptionally induces TRAIL in a p53-independent manner, is a potent caseinolytic protease P (ClpP)  activator with EC50 of 1.25 uM.
ONC201 also is a selective dopamine receptor D2 (DRD2) antagonist.
ONC201 induces a sustained up-regulation of TRAIL in tumors and normal cells, inactivates kinases Akt and ERK, leading to the translocation of Foxo3a into the nucleus.
ONC201 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL.

物理化学性质&存储条件

分子量 386.50
分子式 C24H26N4O
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-10-(2-Methylbenzyl)-2,6,7,8,9,10-hexahydroiMidazo[1,2-a]pyrido[4,3-d]pyriMidin-5(3H)-one

参考文献

1. Allen JE, et al. Sci Transl Med. 2013 Feb 6;5(171):171ra17.

2. Prabhu VV, et al. Cancer Res. 2015 Apr 1;75(7):1423-32.

3. Allen JE, et al. Cancer Res. 2015 Apr 15;75(8):1668-74.

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