1. Neuronal Signaling Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. Utatrectinib

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.

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Utatrectinib Chemical Structure

Utatrectinib Chemical Structure

CAS No. : 1079274-94-4

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Description

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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)
Clinical Trial
Molecular Weight

382.39

Formula

C18H19FN8O

CAS No.
SMILES

CC(C)OC1=CC(N2C=NC3=CC=C(N[C@H](C4=NC=C(F)C=N4)C)N=C32)=NN1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Utatrectinib
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HY-102066
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