larotrectinib
Ligand Summary
Larotrectinib is an inhibitor of the tropomyosin receptor kinases (TRK), TRKA, TRKB, and TRKC. In a broad panel of purified enzyme assays, larotrectinib inhibited TRKA, TRKB, and TRKC with IC50 values between 5-11 nM. One other kinase TNK2 was inhibited at approximately 100-fold higher concentration. TRKA, B, and C are encoded by the genes NTRK1, NTRK2, and NTRK3.Chromosomal rearrangements involving in-frame fusions of these genes with various partners can result in constitutively-activated chimeric TRK fusion proteins that can act as an oncogenic driver, promoting cell proliferation and survival in tumor cell lines.
UNII: PF9462I9HX
PubChem: 46188928
PubChem: 67330085
Guide to Pharmacology: 8909
ChEMBL: CHEMBL3889654
ChEMBL: CHEMBL3989939
DrugCentral: 5305
LyCHI: C82NSTPT86PG
Target Activities
NTRK1
High affinity nerve growth factor receptor
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.01 | |||||
IC50 | 8.7 | J Med Chem, (2019) 62:4:1731 | ||||
IC50 | 8.7 | Eur J Med Chem, (2019) 175:None:129 | ||||
IC50 | 8.48 | Eur J Med Chem, (2019) 179:None:470 | ||||
IC50 | 8.01 | J Med Chem, (2017) 60:1:66 | ||||
IC50 | 8.01 | None, (2014) None:None:None | ||||
IC50 | 8.19 | INHIBITOR | ||||
NTRK3
NT-3 growth factor receptor
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.46 | Eur J Med Chem, (2019) 179:None:470 | ||||
IC50 | 7.62 | J Med Chem, (2017) 60:1:66 | ||||
IC50 | 7.97 | INHIBITOR | ||||
NTRK2
BDNF/NT-3 growth factors receptor
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.28 | Eur J Med Chem, (2019) 179:None:470 | ||||
IC50 | 7.62 | J Med Chem, (2017) 60:1:66 | ||||
IC50 | 8.09 | INHIBITOR | ||||