Home Protein Tyrosine Kinase Trk receptor inhibitor - Apoptosis related activator Larotrectinib sulfate For research use only.

Larotrectinib sulfate

Synonyms: LOXO-101 sulfate, ARRY-470 sulfate

Larotrectinib sulfate 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 sulfate Chemical Structure

Larotrectinib sulfate Chemical Structure

CAS: 1223405-08-0

Selleck's Larotrectinib sulfate has been cited by 21 Publications

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Purity & Quality Control

Batch: Purity: 99.76%
99.76

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KM12 cells Function assay 0, 10, 100, 1000 nM 3 hours LOXO-101 inhibited NTRK1 phosphorylation at 100 nmol/L 28751539
Ba/F3 Function assay 0, 10, 100, 1000 nM 3 hours LOXO-101 inhibited NTRK1 phosphorylation at 100 nmol/L, 28751539
CR20 Function assay 0, 10, 100, 1000 nM 3 hours NTRK1 phosphorylation was inhibited 28751539
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Biological Activity

Description Larotrectinib sulfate 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
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-NTRK(Y490) / p-ERK (T202/Y204) / p-Eif4e pTRKA / TRKA / pTRKC / TRKC / p-AKT / AKT 29568395
Growth inhibition assay Cell proliferation 26216294
In Vivo
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].
Animal Research Animal Models Adult male C3H/HeJ mice
Dosages 10-100 mg/kg
Administration p.o.
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 Recruiting Solid Tumors Harboring NTRK Fusion Bayer September 30 2015 Phase 2

Chemical lnformation & Solubility

Molecular Weight 526.51 Formula

C21H22F2N6O2.H2SO4
CAS No. 1223405-08-0 SDF Download Larotrectinib sulfate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (189.92 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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