1807861-48-8|Onc212|CsnPharm

CAS No.: 1807861-48-8

ONC212 Catalog No. CSN34909

ONC212 is a fluorinated ONC201 analog. It was identified as activator of an orphan GPCR GPR132 and Gαq signaling, which functions as a tumor suppressor.

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技术信息

生物活性

描述ONC212, a fluorinated imipridone, is a novel mitocan targeting oxidative metabolism in pancreatic cancer, leading to different cellular outcomes based on divergent metabolic programs. ONC212 impairs oxidative phosphorylation (OXPHOS) with decrease in mitochondrial-derived ATP production^[1]. ONC212 induced apoptogenic effects through the induction of an integrated stress response, and reduced MCL-1 expression, a known resistance factor for BCL-2 inhibition by ABT-199. Oral administration of ONC212 inhibited AML (human acute myeloid leukemia) growth in vivo and improved overall survival in xenografted mice. Moreover, ONC212 abrogated the engraftment capacity of patient-derived AML cells in an NSG PDX model, suggesting potential eradication of AML initiating cells, and was highly synergistic in combination with ABT-199^[2]. In vivo toxicity assessment experiments show that ONC212 is well tolerated up to 250 mg/kg. 300 mg/kg of ONC212 causes splenic damage and elevates liver enzymes. ONC212 has a slightly shorter half-life than ONC201, with a clearance from the blood at 12 hours, T1/2 of 4.3 hours, and Cmax of 1.4 µg/mL^[3].
参考文献

[1] Ferrarini I, Louie A, Zhou L, El-Deiry WS. ONC212 is a Novel Mitocan Acting Synergistically with Glycolysis Inhibition in Pancreatic Cancer. Mol Cancer Ther. 2021 Sep;20(9):1572-1583
[2] Nii T, Prabhu VV, Ruvolo V, Madhukar N, Zhao R, Mu H, Heese L, Nishida Y, Kojima K, Garnett MJ, McDermott U, Benes CH, Charter N, Deacon S, Elemento O, Allen JE, Oster W, Stogniew M, Ishizawa J, Andreeff M. Imipridone ONC212 activates orphan G protein-coupled receptor GPR132 and integrated stress response in acute myeloid leukemia. Leukemia. 2019 Dec;33(12):2805-2816
[3] Wagner J, Kline CL, Ralff MD, Lev A, Lulla A, Zhou L, Olson GL, Nallaganchu BR, Benes CH, Allen JE, Prabhu VV, Stogniew M, Oster W, El-Deiry WS. 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2703 mL
- 11.3517 mL
- 22.7035 mL
- 5 mM
- 0.4541 mL
- 2.2703 mL
- 4.5407 mL
- 10 mM
- 0.2270 mL
- 1.1352 mL
- 2.2703 mL

技术信息

CAS号	1807861-48-8	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C24H23F3N4O	运输	蓝冰
分子量	440.46	别名

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