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

Utatrectinib  (Synonyms: AZD-7451)

Cat. No.: HY-102066 Purity: 98.72%
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Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.

For research use only. We do not sell to patients.

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.
Appearance

Solid

Color

Blue to blue-green

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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Help & FAQs
  • 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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