Antitumor agent-60

Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Signaling Pathways >> Apoptosis >> MDM-2/p53

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ROS

Signaling Pathways >> MAPK/ERK Pathway >> Raf

Signaling Pathways >> GPCR/G Protein >> Ras

IC50: 12 nM in A549, 19 nM in OVCaR-3, 29 nM in SGC-7901, 22 nM in HCT-116[1] Kd: 721.3 nM (CRAF RBD)[1]

[1]. Liu Z, et al. Targeting RAS-RAF pathway significantly improves antitumor activity of Rigosertib-derived platinum(IV) complexes and overcomes cisplatin resistance. Eur J Med Chem. 2020;194:112269.