Cell cycle is divided into four phases: G1 (gap phase 1), S (DNA synthesis), G2 (gap phase 2), and M (mitosis). Cell cycle progression is regulated by cyclins and their cognate CDKs. As the important regulator of G1 phase, CDK4/6 inhibitors have been developed, for example, PD-0332991 (palbociclib), LY2835219 (abemaciclib), and LEE011 (ribociclib) that are approved by U.S. Food and Drug Administration to treat human tumors.