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IHMT-TRK-284

Names

[ CAS No. ]:
2416844-79-4

[ Name ]:
IHMT-TRK-284

Biological Activity

[Description]:

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

[Target]

TrkB:0.7 nM (IC50)

TrkC:2.6 nM (IC50)

TrkA:10.5 nM (IC50)

PDGFRα:24.2 nM (IC50)

PDGFRβ:95.7 nM (IC50)

Abl1:83.6 nM (IC50)

CSF1R:1.2 nM (IC50)

KIT:2167 nM (IC50)


[References]

[1]. Beilei Wang, et al. Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants. Eur J Med Chem. 2020 Dec 1;207:112744.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H27N7OS

[ Molecular Weight ]:
473.59

Related Compounds