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ON1231320
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ON1231320图片
CAS NO:1312471-39-8
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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。
Cas No.1312471-39-8
分子式C22H15F2N5O3S
分子量467.45
溶解度DMSO : 25 mg/mL (53.48 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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[1][2].

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].

ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth[1].

[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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