Larotrectinib, TRK inhibitor (pan)

Product Details

Formal 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

Molecular Formula: C₂₁H₂₂F₂N₆O₂

Formula Weight: 428.44

CAS Number: 1223403-58-4

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 5 mg/ml)

Storage: RT

Stability: ≥ 1 year.

Applications

TRK inhibitor (pan)

Functions

Potent (IC50’s < 11 nM) inhibitor of tropomyosin receptor kinases A, B, and C (TrkA, B, and C). It is >100 fold selective against a panel of 229 kinases. Markedly attenuats bone cancer pain, and significantly blocks formation of neuroma-like structures and the sprouting of sensory nerve fibers. Larotrectinib caused substantial tumor regression in various cancers displaying TRK gene fusions and is the first tissue agnostic cancer drug approved by the FDA.

Application Procedures

First dissolved in DMSO (up to 5 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 2 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)