Home Protein Tyrosine Kinase Trk receptor inhibitor Larotrectinib For research use only.

Larotrectinib

Synonyms: Vitrakvi, LOXO-101, ARRY-470

Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.

Larotrectinib Chemical Structure

Larotrectinib Chemical Structure

CAS No. 1223403-58-4

Purity & Quality Control

Larotrectinib Related Products

Signaling Pathway

Trk receptor Signaling Pathways

Trk receptor Signaling Pathway

Biological Activity

Description Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.
Targets
TRK [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04655404 Recruiting
High Grade Glioma|Diffuse Intrinsic Pontine Glioma
Nationwide Children''s Hospital
 April 8 2021 Early Phase 1
NCT04814667 Active not recruiting
Solid Tumor Adult|Locally Advanced Solid Tumor|Metastatic Cancer
Centre Leon Berard|Bayer
 February 23 2021 --
NCT04142437 Recruiting
Locally Advanced or Metastatic Solid Tumor Harboring an NTRK Gene Fusion
Bayer
 April 3 2020 --
NCT03834961 Active not recruiting
Central Nervous System Neoplasm|Infantile Fibrosarcoma|Recurrent Acute Leukemia|Refractory Acute Leukemia|Solid Neoplasm
Children''s Oncology Group|National Cancer Institute (NCI)
 October 25 2019 Phase 2
NCT02637687 Active not recruiting
Solid Tumors Harboring NTRK Fusion
Bayer
 December 16 2015 Phase 1|Phase 2
NCT02576431 Active not recruiting
Solid Tumors Harboring NTRK Fusion
Bayer
 September 30 2015 Phase 2

Chemical Information & Solubility

Molecular Weight 428.44 Formula
C21H22F2N6O2
CAS No. 1223403-58-4 SDF --
Smiles OC1CCN(C1)C(=O)NC2=C3N=C(C=C[N]3N=C2)N4CCCC4C5=CC(=CC=C5F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (200.72 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


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Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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