计算溶液所需的质量、体积或浓度。
概述
ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC 50 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
In Vitro
ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC 50 >10 µM). ON1231320 (0-5 µM; 24 hours) activates programmed cell death in human tumor cells. ON1231320 inhibits cell proliferation in 16 tumor cell lines (DU145, MCF-7, BT474, SK-OV-3, MIA-PaCa-2, SK-MEL-28, A549, U87, COLO-205, HELA, H1975, RAJI, U205, K562, GRANTA-519; IC 50 = 0.035-0.2 µM). ON1231320 does not appreciably inhibit tubulin polymerization. ON1231320 does not affect normal human fibroblasts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: U2OS cells Concentration: 0-5 µM Incubation Time: 24 hours Result: Increased the activity of Caspases 3/7 in a dose-dependent manner. Induced apoptosis.
In Vivo
ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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%)
Form:Solid
IC50& Target:PLK2 0.31 μM (IC 50 ) PLK1 >10 μM (IC 50 ) PLK3 >10 μM (IC 50 ) PLK4 >10 μM (IC 50 )
规格
规格或纯度
≥99%
英文名称
ON1231320
生化机理
ON1231320是一种高度特异性的polo like kinase 2（PLK2）抑制剂，IC 50为0.31 µM。ON1231320能阻断有丝分裂G2/M期的肿瘤细胞周期进程，导致细胞凋亡。ON1231320是一种芳基磺酰基吡啶嘧啶酮，具有抗抑郁、抗肿瘤和抗衰老作用。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
467.45
高级数据
化学和物理性质
溶解性
DMSO : 25 mg/mL (53.48 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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溶液计算器
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