TRK-IN-24

Names

[ CAS No. ]:
2937544-01-7

[ Name ]:
TRK-IN-24

Biological Activity

[Description]:

TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKAG595R, TRKAG667C and TRKAF589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM[1].

[Related Catalog]:

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

[Target]

IC50: 5.21 nM (TRKA), 4.51 nM (TRKC), 6.77 nM (TRKAG595R), 1.42 nM (TRKAG667C), 6.13 nM (TRKAF589L)[1]


[References]

[1]. Wang Z, et al. Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations. J Med Chem. 2023 Sep 7.. .  

Chemical & Physical Properties

[ Molecular Formula ]:
C39H45N7O3

[ Molecular Weight ]:
659.82

Related Compounds