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TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKAG595R, TRKAF589L, and TRKAG667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells[1]. | [IC 50]
TrkA: 0.5 nM (IC50); TrkC: 9 nM (IC50); TRKAG595R: 14 nM (IC50); TRKAF589L: 4.4 nM (IC50); TRKAG667C: 4.8 nM (IC50) | [References]
[1] Qiaohua Qin, et al. Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors. Eur J Med Chem. 2023 May 5;253:115291. DOI:10.1016/j.ejmech.2023.115291 |
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