Integrin-IN-2

Names

[ CAS No. ]:
2378617-67-3

[ Name ]:
Integrin-IN-2

Biological Activity

[Description]:

Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cytoskeleton >> Integrin

[Target]

pIC50: 7.8 (αvβ6), 8.4 (αvβ3), 8.4 (αvβ5) and 7.4 (αvβ8)[1]


[In Vivo]

In vivo pharmacokinetic studies in CD rats revealed that racemic Integrin-IN-2 (compound 39) has a low plasma clearance of 8 mL/(min kg), a low to moderate volume of distribution of 0.5 L/kg, a moderate halflife of 1.8 h, and very high bioavailability of 98%[1].

[References]

[1]. Anderson NA, et al. Discovery of an Orally Bioavailable Pan αv Integrin Inhibitor for Idiopathic Pulmonary Fibrosis. J Med Chem. 2019 Oct 10;62(19):8796-8808.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H30N4O3

[ Molecular Weight ]:
458.55

Related Compounds