LOXO-195 (SELITRECTINIB)

Background Information:

Selitrectinib (LOXO-195) is an oral, second generation TRK inhibitor
being made to address the acquired resistance to first generation TRK
inhibitor (such as LOXO-101). LOXO-195 potently and selectively
inhibits, with minimal activity against other kinases, pan-TRKs (with
potency on par with that of LOXO-101), and more importantly, abrogates
resistance in TRK fusion–positive cancers that acquired kinase domain
mutations due to the treatment of existing TRK inhibitors. Displays high
oral bioavailability and favorable PK in animals.

Reference:

1. A. Drilon, et al. A Next-Generation TRK Kinase Inhibitor Overcomes
Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK
Fusion Positive Solid Tumors. Cancer Discov. 2017 Sep;7(9):963-972.

APIM050184: LOXO-195 (SELITRECTINIB)

CAS No.: 2097002-61-2.
Molecular Formula: C20H21FN6O.
Molecular Weight: 380.4.
Purity: >99.5% chemical and optical purity by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.