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Product Details

Larotrectinib | Potent and selective panTRK inhibitor

Larotrectinib (1223403-58-4) is a potent (IC50’s < 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.

References/Citations
1) Ghilardi et al. (2010), Administration of a tropomyosin receptor kinase inhibitor attenuates sarcoma-induced nerve sprouting, neuroma formation, and bone cancer pain; Mol. Pain, 6 87
2) Doebele et al. (2015), An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101; Cancer Discov., 5 1049
3) Landman et al. (2018), Rapid response to Larotrectinib (LOXO-101) in Adult Chemotherapy-Naïve Patients With Advanced Triple-Negative Secretory Breast Cancer Expressing ETV6-NTRK3 Fusion; Clin. Breast Cancer, 18 e267
4) Drilon et al. (2018), Efficacy of Larotrectinib in TRK Fusion-Positive Cancers in Adults and Children; N. Engl. J. Med., 378 731

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Catalog#  10-4832-0005

$65.00
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CAS:
1223403-58-4
Catalog Number:
10-4832
Activity:
Potent and selective panTRK inhibitor
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 Name:
LOXO-101; ARRY-470
Molecular Weight:
428.44
Molecular Formula:
C21H22F2N5O2
Solubility:
Soluble in DMSO (up to 5 mg/ml).
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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