Larotrectinib | TRK inhibitor

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$60.00
25 mg$225.00

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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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