ON1231320 是一种高度特异性的 polo 样激酶 2 (PLK2) 抑制剂，IC50为 0.31 μM。ON1231320 在有丝分裂 G2/M 期阻断肿瘤细胞周期进程，导致细胞凋亡。ON1231320 是一种芳基磺酰基吡啶并嘧啶酮，具有抗肿瘤活性。
| 生物活性 | ON1231320 is a highly specificpolo like kinase 2 (PLK2)inhibitor with anIC50of 0.31 μM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causingapoptoticcell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity[1][2]. |
| IC50& Target[1] | PLK2 0.31 μM (IC50) | PLK1 >10 μM (IC50) | PLK3 >10 μM (IC50) | PLK4 >10 μM (IC50) |
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体外研究
(In Vitro) | ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC50>10 μM)[1].
ON1231320 (0-5 μM; 24 hours) activates programmed cell death in human tumor cells[1].
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; IC50= 0.035-0.2 μM)[1].
ON1231320 does not appreciably inhibit tubulin polymerization[1]. ON1231320 does not affect normal human fibroblasts[2].
Apoptosis Analysis[1] | Cell 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. |
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体内研究
(In Vivo) | ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth[1].
| Animal Model: | 6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells[1] | | Dosage: | 75 mg/kg | | Administration: | IP; alternate days (Q2D) for 20 days | | Result: | Resulted in significant inhibition of tumor growth (86.5%) |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(53.48 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1393 mL | 10.6963 mL | 21.3927 mL | | 5 mM | 0.4279 mL | 2.1393 mL | 4.2785 mL | | 10 mM | 0.2139 mL | 1.0696 mL | 2.1393 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (5.35 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.35 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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