PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research.
PLK1/BRD4-IN-5 (Compound SC10) shows significant anti-proliferation activity against all three tumor cell lines (MDA-MB-231 IC50 = 17.3 nM, MDA-MB-361 IC50 = 8.4 nM, MV4-11 IC50 = 5.4 nM)[1].
Pharmacokinetic parameters of compounds in Sprague-Dawley Rats [1]
References:
[1]. Liu J, et al. Discovery and optimization of didropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer. Bioorg Med Chem. 2024;101:117