Product Name: LOXO-101
 CAT#: A-9048

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 Synonym:LOXO-101 ,

LOXO-101 Chemical Structure
LOXO-101chemical structure

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IUPAC/Chemical name:

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Biological Activity
LOXO-101 is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons. Translocations involving the TRK kinase domain, mutations involving the TRK ligand-binding site, amplifications of NTRK, TRK splice variants, and autocrine/paracrine signaling are described in diverse tumor types, and may contribute to tumorigenesis. LOXO-101 is currently being developed by Loxo Oncology, Inc.
Technical Data

Purity: >99%
Chemical Formula:C21H22F2N6O2
Molecular Weight:428.44

IUPAC/Chemical name: (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
Canonical SMILES: O=C(N1CC[C@@H](C1)O)NC2=C3N=C(N4CCC[C@@H]4C5=CC(F)=CC=C5F)C=CN3N=C2

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