ON1231320,99.24%

产品编号:Bellancom-100789| CAS NO:1312471-39-8| 分子式:C22H15F2N5O3S| 分子量:467.45

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-100789
1000.00 杭州 北京(现货)
Bellancom-100789
1700.00 杭州 北京(现货)
Bellancom-100789
3500.00 杭州 北京(现货)
Bellancom-100789
5500.00 杭州 北京(现货)
Bellancom-100789
9500.00 杭州 北京(现货)

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ON1231320

产品介绍 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 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.

体外研究

ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC50>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; IC50= 0.035-0.2 µM).
ON1231320 does not appreciably inhibit tubulin polymerization. ON1231320 does not affect normal human fibroblasts.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis

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.

西域 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%)
体内研究

ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth.

西域 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%)
体内研究

ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth.

西域 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%)
性状Solid
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 西域 网站选购。
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
参考文献

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