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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.
APIM050039: 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.
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