LAROTRECTINIB

LAROTRECTINIB : Inhibitor of NTRK1, NTRK2, NTRK3

Structure

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Information

NTRK1
NTRK2
NTRK3

Inhibitor

up to 250 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P04629

Target Class: Kinase

Target SubClass: Tyr kinase

Potency: IC50

Potency Value: 1.2 nM

Potency Assay: Activity assay using 10 µM ATP

PDB ID for probe-target interaction (3D structure): --

Target aliases:

High affinity nerve growth factor receptor, TRKA, ...

DOI Reference: 10.1016/j.bmcl.2020.127712

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Within target family: Broad radiometric protein screen to determine the selectivity of a Trk inhibitor (ARRY-470) vs. a diverse panel of kinases. Trk inhibitor ARRY-470 is > 100 fold selective when tested against a diverse panel of 229 radiometric protein kinases (DOI: 10.1038/nm.3352). Outside target family: A broad radioligand screen to determine the selectivity of a Trk inhibitor (ARRY-470) vs. a diverse panel of receptors, channels, and transporters. Trk inhibitor ARRY-470 is > 1000 fold selective when tested against a diverse panel of receptors, channels, and transporters. The Trk inhibitor ARRY-470 does not show any significant inhibition against this panel of receptors.

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(last updated: 31 May 2023 )