ON1231320

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ON1231320  纯度: 99.24%

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。

ON1231320

ON1231320 Chemical Structure

CAS No. : 1312471-39-8

规格 价格 是否有货 数量
5 mg ￥1000 In-stock
10 mg ￥1700 In-stock
25 mg ￥3500 In-stock
50 mg ￥5500 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

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ON1231320 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

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[1][2].

IC50 & Target[1]

PLK2

0.31 μM (IC50)

PLK1

>10 μM (IC50)

PLK3

>10 μM (IC50)

PLK4

>10 μM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 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[1]
Dosage: 75 mg/kg
Administration: IP; alternate days (Q2D) for 20 days
Result: Resulted in significant inhibition of tumor growth (86.5%)

分子量

467.45

Formula

C22H15F2N5O3S
CAS 号

1312471-39-8
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
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (53.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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