1079274-94-4

1079274-94-4 structure

Name: Utatrectinib
Chemical Name: AZD-7451
CAS Number: 1079274-94-4
Molecular Formula: C₁₈H₁₉FN₈O
Molecular Weight: 382.395
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Trk Receptor
Create Date: 2018-08-06 20:01:04
Modify Date: 2024-03-07 09:09:57
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors[1].

Name	AZD-7451
Synonyms	3H-Imidazo[4,5-b]pyridin-5-amine, N-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-3-[5-(1-methylethoxy)-1H-pyrazol-3-yl]- AZD-7451 N-[(1S)-1-(5-Fluoro-2-pyrimidinyl)ethyl]-3-(5-isopropoxy-1H-pyrazol-3-yl)-3H-imidazo[4,5-b]pyridin-5-amine VNM956Y27V

Description	Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor
In Vitro	Utatrectinib (100 nM, 22 h) inhibits the migration of TrkC-expressing U2SO cells[2]. Utatrectinib (1-10 nM, 24 h) inhibits cell growth in KM12, H460 and H810 cells[3]. Utatrectinib (5 nM, 24 h) inhibits phosphorylation of TRKA/B and downstream signaling in KM12, H460 cells[3]. Cell Migration Assay [2] Cell Line: TrkC-expressing U2SO cells Concentration: 100 nM Incubation Time: 22 h Result: Inhibited cell migration (~2.3-fold, P<0.01). Western Blot Analysis[3] Cell Line: KM12, H460 cells Concentration: 0, 1, 5 nM Incubation Time: 24 h Result: Inhibited pTRKA Tyr490 and pAk in KM12 cells. Inhibited pTRKB Tyr706/707 and pERK in H460 cells.
In Vivo	Utatrectinib (50 mg/kg, p.o., daily) suppresses adenoid cystic carcinoma (ACC) tumor growth in ACCX6 xenograft nu/nu mice model[2]. Animal Model: Xenograft nu/nu mice models of human ACC: ACCX6 and ACCX9[2] Dosage: 50 mg/kg Administration: Oral administration, daily. Result: Tumor growth inhibition (TGI): 64% (in ACCX6 model)