cdk2-in-45

CDK2-IN-45 is a CDK2 inhibitor with an IC50 value of 0.64 μM. It effectively inhibits the proliferation of DU-145 and PC-3 cell lines, with IC50 values of 2.20 μM and 4.17 μM, respectively. Additionally, CDK2-IN-45 induces G0/G1 phase cell cycle arrest and apoptosis. It is utilized in prostate cancer research.

ALK/PI3K/AKT-IN-1 (Compound 45) effectively inhibits the proliferation of cancer cell lines A549, H1975, and PC9, with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound enhances the expression of p21 and p27, and decreases the activity of CDK2 and p-Rb, causing cell cycle arrest at the G1 phase. It suppresses the ALK/PI3K/AKT signaling pathway, promotes mitochondrial membrane potential depolarization, and induces apoptosis in A549 cells. Furthermore, ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheres.

EGFR-IN-45 is a potent pan-inhibitor of the epidermal growth factor receptor (EGFR) with an IC50 of 0.4 μM and also targets CDK2 with an IC50 of 1.6 μM. It inhibits topoisomerases Topo I and Topo II, blocks the cancer cell cycle in the pre-G1 phase, and induces apoptosis.

CDK/HDAC-IN-2 is a potent dual HDAC/CDK inhibitor that acts on HDAC1 (IC50: 6.4 nM), HDAC2 (IC50: 0.25 nM), HDAC3 (IC50: 45 nM), HDAC6 and 8 (IC50 > 1000 nM), CDK1 (IC50: 8.63 nM), CDK2 (IC50: 0.30 nM), and CDK4, 6, and 7 (IC50 > 1000 nM). CDK/HDAC-IN-2 can arrest the cell cycle in the G2/M phase and induce apoptosis, demonstrating excellent anti-proliferative and significant anti-tumor effects.

QR-6401, a selective macrocyclic CDK2 inhibitor, is orally active with IC50 values of 0.37 nM for CDK2/E1, 10 nM for CDK9/T1, 22 nM for CDK1/A2, 34 nM for CDK6/D3, and 45 nM for CDK4/D1. It exhibits potent antitumor activity in the OVCAR3 ovarian cancer xenograft model, indicating its potential for use in cancer research [1].