ON-013100

ON-013100,一种抗肿瘤药物,作为有丝分裂的抑制剂,能够抑制细胞周期蛋白 D1 (Cyclin D1) 的表达。

研究领域 >> 癌症

Cdk4/cyclin D1

ON-013100诱导细胞凋亡,并且在体外具有针对大多数人癌细胞系的活性。 ON013100显着改变细胞周期谱,显着增加G2/M期细胞数。用甚至0.1μM的ON013100处理细胞导致细胞周期的G2/M期停滞[2]。 ON 013100以纳摩尔浓度抑制MCL(JEKO-1和MINO),乳腺(MCF7和MDA-MB-231),胃(AGS)和食道(OE19,OE33和FLO-1)癌细胞系的增殖(ON 013100 GI50 = 6.7-11.2 nM)[3]。

[1]. Cho SY, et al. Determination of the glucuronide metabolite of ON 013100, a benzylstyrylsulfone antineoplastic drug, in colon cancer cells using LC/MS/MS. J Pharm Biomed Anal. 2013 Mar 5;75:138-44.

[2]. Park IW, et al. Evaluation of novel cell cycle inhibitors in mantle cell lymphoma. Oncogene. 2007 Aug 16;26(38):5635-42.

[3]. Neel Jasani, et al. Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

N-[5-[(4-乙基-1-哌嗪基)甲基]-2-吡啶基]-5-氟-4-[4-氟-2-甲基-1-异丙基-1H-苯并咪唑-6-基]-2-嘧啶胺甲烷磺酸盐 | 瑞博西尼 | Dinaciclib | THZ1 | Roscovitine | THZ531 | 2-[[(噻吩-2-基)甲基]氨基]-5-[1-(喹啉-6-基)甲-(Z)-亚基]噻唑-4-酮 | 夫拉平度 | NVP-2 | 阿维西利 | CYC065 | 4-[2-甲基-1-异丙基-1H-咪唑-5-基]-N-[4-(甲磺酰基)苯基]-2-嘧啶胺 | GSK 3抑制剂IX | 肯帕罗酮 | SNS-032 (BMS-387032)