DDR1-IN-6

Names

[ CAS No. ]:
2416021-47-9

[ Name ]:
DDR1-IN-6

Biological Activity

[Description]:

DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 9.7 nM. DDR1-IN-6 has anti-cancer activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Discoidin Domain Receptor

[Target]

DDR1:9.72 nM (IC50)


[In Vitro]

DDR1-IN-6 (compound 1; for 24 hours) inhibits collagen production in human hepatic stellate cell LX-2 (IC50=13 nM)[1]. DDR1-IN-6 (72 hours) has cytotoxicity in LX-2 cells (CC50=3 μM)[1]. DDR1-IN-6 (0-30 μM) has anti-proliferation effects on primary tumor cells freshly isolated from PC-07-0024 (IC50=5.7 μM of 3 days; IC50=2.65 μM of 6 days) and LU-01-0523 derived xenograft (PDX) tumor model (IC50>30 μM of 3 days; IC50>30 μM of 6 days)[1].

[References]

[1]. Aleksandr M. Aliper, et al. Kinase inhibitors. WO2020079652A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H14F3N5O

[ Molecular Weight ]:
433.39


Related Compounds