Antitumor agent-60

Names

[ CAS No. ]:
865784-65-2

[ Name ]:
Antitumor agent-60

Biological Activity

[Description]:

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].

[Related Catalog]:

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

[Target]

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]


[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H28O10S

[ Molecular Weight ]:
508.54

Related Compounds