CDKI-73

CDKI-73是CDK9高效抑制剂,Ki值为4nM,对CLL细胞株有选择性毒性作用,LD50值为80nM,对正常B细胞作用基本无。

研究领域 >> 癌症

CDK2:3.27 nM (IC50)

CDK9:5.78 nM (IC50)

CDK1:8.17 nM (IC50)

CDK4:8.18 nM (IC50)

CDK6:37.68 nM (IC50)

CDK7:134.26 nM (IC50)

[1]. Xie S, et al. Antitumor action of CDK inhibitor LS-007 as a single agent and in combination with ABT-199 against human acute leukemia cells. Acta Pharmacol Sin. 2016 Nov;37(11):1481-1489.

[2]. Lam F, et al. Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73. Oncotarget. 2014 Sep 15;5(17):7691-704.

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)