| Identification | Back Directory | [Name]
1-Piperazineacetamide, 4-methyl-N-[4-methyl-5-[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]-2-thiazolyl]- | [CAS]
2416844-79-4 | [Synonyms]
IHMT-TRK-284
1-Piperazineacetamide, 4-methyl-N-[4-methyl-5-[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]-2-thiazolyl]- | [Molecular Formula]
C25H27N7OS | [MOL File]
2416844-79-4.mol | [Molecular Weight]
473.59 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
TrkB: 0.7 nM (IC50); TrkC: 2.6 nM (IC50); TrkA: 10.5 nM (IC50); CSF1R: 1.2 nM (IC50); PDGFRα: 24.2 nM (IC50); PDGFRβ: 95.7 nM (IC50); Abl1: 83.6 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 resistan DOI:10.1016/j.ejmech.2020.112744 |
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