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首页-小分子抑制剂&激动剂-Others-Other Targets-ONC212
ONC212

Chemical Structure : ONC212

CAS No.: 1807861-48-8

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ONC212 (ONC-212)

货号: PC-72443Not For Human Use, Lab Use Only.

ONC212 (ONC-212) is a potent anti-cancer small molecule, activator of an orphan GPCR GPR132 and Gαq signaling, also is a potent activator of ClpP activator with EC50 of 131 nM.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 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

ONC212 (ONC-212) is a potent anti-cancer small molecule, activator of an orphan GPCR GPR132 and Gαq signaling, also is a potent activator of ClpP activator with EC50 of 131 nM.
ONC212 possesses highly increased antitumor activity compared to the first-generation compound ONC201.
ONC212 induced apoptogenic effects through the induction of an integrated stress response, and reduced MCL-1 expression.
Oral administration of ONC212 inhibited AML growth in vivo and improved overall survival in xenografted mice.
ONC212 exhibited broad-spectrum efficacy at nanomolar concentrations across solid tumors and hematological malignancies.
ONC212 impairs oxidative phosphorylation (OXPHOS) with decrease in mitochondrial-derived ATP production, mitochondrial protease ClpP was identified as an ONC212-binding target.

物理化学性质&存储条件

分子量 440.47
分子式 C24H23F3N4O
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

100 mM in DMSO (44 mg/mL)
Chemical Name/SMILES

2,4,6,7,8,9-Hexahydro-7-(phenylmethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one

参考文献

1. Nii T, et al. Leukemia. 2019 Dec;33(12):2805-2816.

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

3. Lev A, et al. Oncotarget. 2017 Sep 12;8(47):81776-81793.

4. Ferrarini I, et al. Mol Cancer Ther. 2021 Sep;20(9):1572-1583.

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