Molfile
Inchi
Smiles
Synonyms:
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larotrectinib
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vitrakvi
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LOXO-101
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ARRY-470
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larotrectinib sulfate
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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.
- Molecular weight: 428.44
- Formula: C21H22F2N6O2
- CLOGP: 2.70
- LIPINSKI: 0
- HAC: 8
- HDO: 2
- TPSA: 86
- ALOGS: -3.26
- ROTB: 3
- Status: ONP
Legend: OFP - off patent OFM - off market ONP - on patent
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