| 产品描述: | ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity |
| 靶点: |
PLK2:0.31 μM (IC50);PLK1:>10 μM (IC50);PLK3:>10 μM (IC50);PLK4:>10 μM (IC50);Apoptosis; PLK |
| 体内研究: |
ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth. Animal Model: 6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells Dosage: 75 mg/kg Administration: IP; alternate days (Q2D) for 20 days Result: Resulted in significant inhibition of tumor growth (86.5%) |
| 参考文献: |
1. M V Ramana Reddy, et al. Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2). Bioorg Med Chem. 2016 Feb 15;24(4):521-44. 2. Shashidhar S. Jatiani, et al. Abstract 643: Targeting cancer with a selective ATP-mimetic inhibitor of polo like kinase-2. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
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| 注意: |
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