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Larotrectinib

Catalog No. T5995 CAS 1223403-58-4

Synonyms: LOXO-101, ARRY-470

Larotrectinib 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

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	Larotrectinib 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 2 years

Solubility Information

DMSO: 4.6 mg/mL (10.74 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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