Chemical Name: (3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)pyrrolidine-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide. Alternate Names: LOXO-101, ARRY-470
panTRK inhibitor
Molecular Weight:
428.44
Purity:
98% by HPLC NMR (Conforms)
Form:
Yellow solid
CAS Number:
[1223403-58-4]
Formula:
C21H22F2N6O2
Application Notes:
Larotrectinib is a potent (IC50s < 11 nM) inhibitor of tropomyosin receptor kinases A, B, and C (TrkA, B, and C).1 It is >100 fold selective against a panel of 229 kinases. Larotrectinib markedly attenuated bone cancer pain and significantly blocked the formation of neuroma-like structures and the sprouting of sensory nerve fibers. Larotrectinib caused substantial tumor regression in various cancers displaying TRK gene fusions.2-4 Larotrectinib is the first tissue agnostic drug approved by the FDA.
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