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Larotrectinib

Catalog No. T5995 CAS 1223403-58-4

Synonyms: LOXO-101, ARRY-470

Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors(IC50s = 2-20 nM).

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Larotrectinib, CAS 1223403-58-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 48.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
50 mg	In stock	$ 265.00
100 mg	In stock	$ 397.00
1 mL * 10 mM (in DMSO)	In stock	$ 78.00

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Purity: 100%

Biological Description

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Description	Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors(IC50s = 2-20 nM).
Targets&IC50	Trk:2-20 nM
In vivo	In vivo, Larotrectinib?(60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model[1].
Animal Research	Mice were maintained under aseptic conditions.?The care and treatment of experimental animals was in accordance with institutional guidelines.?5 × 10^5 KM12 cells were injected subcutaneously into the dorsal flank area of the mice.?Tumor volume was monitored by direct measurement with calipers and calculated by the formula: length × (width^2)/2.?Following the establishment of tumor and when the tumor size was between 150–200 mm^2, mice were randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib(LOXO-101).?LOXO-101 was administered by oral gavage once daily for 14 days.?After the last dose, tissue and blood were collected at 3, 6 and 24 hours post-treatment[1].

Synonyms	LOXO-101, ARRY-470
Molecular Weight	428.44
Formula	C21H22F2N6O2
CAS No.	1223403-58-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.6 mg/mL (10.74 mM)

References and Literature

1. Doebele R C , Davis L E , Vaishnavi A , et al. An oncogenic NTRK fusion in a soft tissue sarcoma patient with response to the tropomyosin-related kinase (TRK) inhibitor LOXO-101[J]. Cancer Discovery, 2015, 5(10):1049-1057. 2. Laetsch T W , Dubois S G , Mascarenhas L , et al. Larotrectinib for paediatric solid tumours harbouring NTRK gene fusions: phase 1 results from a multicentre, open-label, phase 1/2 study[J]. The Lancet Oncology, 2018:S1470204518301190.

Citations

1. Jin X, Liu D, Zhou X, et al.Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7.Cell Reports Medicine.2023, 4(12).

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Highly Selective Inhibitor Library EMA Approved Drug Library Clinical Compound Library

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Keywords

Larotrectinib 1223403-58-4 Apoptosis Tyrosine Kinase/Adaptors Trk receptor Trk Receptor LOXO101 ARRY 470 ARRY470 LOXO-101 inhibit Inhibitor ARRY-470 Tropomyosin related kinase receptor LOXO 101 inhibitor

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