Larotrectinib (LOXO-101) sulfate

Catalog No.S7960 Synonyms: ARRY-470, Larotrectinib

For research use only.

Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.

Larotrectinib (LOXO-101) sulfate Chemical Structure

CAS No. 1223405-08-0

Selleck's Larotrectinib (LOXO-101) sulfate has been cited by 15 publications

Purity & Quality Control

Choose Selective Trk receptor Inhibitors

Biological Activity

Description Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.
Targets
TRK [1]
()
In vitro

ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KM12 cells M4HNO2Z2dmO2aX;uJIF{e2G7 M{C5bFAtKDFyLDCxNFAtKDFyMECgcm0> NUjHbWQ4OyCqb4Xydy=> NFqxWHJNV1iRLUGwNUBqdmirYnn0[YQhVlSUS{GgdIhwe3Cqb4L5cIF1cW:wIHH0JFExOCCwbX;sM2w> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd3MUWzPUc,Ojh5NUG1N|k9N2F-
Ba/F3 MUjGeY5kfGmxbjDhd5NigQ>? MXywMEAyOCxiMUCwMEAyODByIH7N MoHaN{Bpd3W{cx?= NVzSWplFVE:[Tz2xNFEhcW6qaXLpeIVlKE6WUluxJJBpd3OyaH;yfYxifGmxbjDheEAyODBibn3vcE9NNA>? MlTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5NUG1N|koRjJ6N{WxOVM6RC:jPh?=
CR20 Mn\DSpVv[3Srb36gZZN{[Xl? M4\MeFAtKDFyLDCxNFAtKDFyMECgcm0> M{DK[lMhcG:3coO= MmPYUnRTUzFicHjvd5Bpd3K7bHH0bY9vKHejczDpcohq[mm2ZXS= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDd3MUWzPUc,Ojh5NUG1N|k9N2F-
Assay
Methods Test Index PMID
Western blot p-NTRK(Y490) / p-ERK (T202/Y204) / p-Eif4e ; pTRKA / TRKA / pTRKC / TRKC / p-AKT / AKT 29568395 26216294
Growth inhibition assay Cell proliferation 26216294
In vivo Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier[1].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: Ba/F3 cells
  • Concentrations: 10, 100, 1000 nM
  • Incubation Time: 5 h
  • Method: Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G, gefitinib 1,000 nM) or DMSO control. The cell lysate are used for western bolt analysis.
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: Adult male C3H/HeJ mice
  • Dosages: 10-100 mg/kg
  • Administration: p.o.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(189.92 mM)
Water Insoluble
Ethanol '100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 526.51
Formula

C21H22F2N6O2.H2SO4

CAS No. 1223405-08-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(N(C1)C2=NC3=C(C=NN3C=C2)NC(=O)N4CCC(C4)O)C5=C(C=CC(=C5)F)F.OS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04655404 Recruiting Drug: Larotrectinib|Procedure: Larotrectinib High Grade Glioma Nationwide Children''s Hospital April 8 2021 Early Phase 1
NCT04814667 Recruiting -- Solid Tumor Adult|Locally Advanced Solid Tumor|Metastatic Cancer Centre Leon Berard|Bayer February 23 2021 --
NCT04142437 Recruiting Drug: larotrectinib(Vitrakvi BAY2757556) Locally Advanced or Metastatic Solid Tumor Harboring an NTRK Gene Fusion Bayer April 3 2020 --
NCT03834961 Recruiting Drug: Larotrectinib Sulfate Central Nervous System Neoplasm|Infantile Fibrosarcoma|Recurrent Acute Leukemia|Refractory Acute Leukemia|Solid Neoplasm Children''s Oncology Group|National Cancer Institute (NCI) September 18 2019 Phase 2
NCT02637687 Recruiting Drug: Larotrectinib (Vitrakvi BAY2757556) Solid Tumors Harboring NTRK Fusion Bayer December 16 2015 Phase 1|Phase 2
NCT02576431 Recruiting Drug: BAY2757556 (Larotrectinib Vitrakvi) Solid Tumors Harboring NTRK Fusion Bayer September 30 2015 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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