Larotrectinib (LOXO-101) sulfate

Catalog No.S7960 Synonyms: ARRY-470, Larotrectinib

Larotrectinib (LOXO-101) sulfate Chemical Structure

Molecular Weight(MW): 526.51

Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

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2 Customer Reviews

  • Quantification of colony formation in (A), shown as a percentage of the control for NCIH2077 and RT112. Mean (3 biological replicates) +/- standard deviation (SD) shown (* p-value < 0.05, ** < 0.005, *** < 0.0005, two-sided t-test, comparing combination treatment to BGJ398 treatment). ns = not significant. (BGJ, BGJ398; Tram, Trametinib; BKM, BKM120; AZD, 8931; LDC, LDC1267; LOXO, LOXO-101; Imat, Imatinib; MGCD, MGCG-265).

    molecular cancer therapeutics. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

    Inhibition of TRKA phosphorylation by Larotrectinib in NGF stimulated HEK293 cells. X-axis denotes concentrations of larotrectinib in nM. Y-Axis denotes percent inhibition of TRKA phosphorylation. Average IC50 of larotrectinib was found to be 10.9 nM. NGF: Neurite growth factor.

    Analytical Biochemistry, 2018, 545(15):78-83. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

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Biological Activity

Description Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
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].

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

Cell Research:[2]
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  • 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]
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  • Animal Models: Adult male C3H/HeJ mice
  • Formulation: Labrafac;polygly-colyzed glyceride
  • Dosages: 10-100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

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

* 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 powder
in solvent
Synonyms ARRY-470, Larotrectinib

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03213704 Recruiting Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|Malignant Glioma|NTRK1 Fusion Positive|NTRK2 Fusion Positive|NTRK3 Fusion Positive|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Refractory Central Nervous System Neoplasm|Refractory Childhood Malignant Germ Cell Tumor|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Solid Neoplasm|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Rhabdoid Tumor|Stage III Osteosarcoma AJCC v7|Stage III Soft Tissue Sarcoma AJCC v7|Stage IV Osteosarcoma AJCC v7|Stage IV Soft Tissue Sarcoma AJCC v7|Stage IVA Osteosarcoma AJCC v7|Stage IVB Osteosarcoma AJCC v7|Wilms Tumor National Cancer Institute (NCI) July 24 2017 Phase 2
NCT02637687 Recruiting Neoplasms|Central Nervous System Neoplasms Loxo Oncology Inc.|Bayer December 2015 Phase 1|Phase 2
NCT02576431 Recruiting Carcinoma Non-Small-Cell Lung|Thyroid Neoplasms|Sarcoma|Colorectal Neoplasms|Salivary Gland Neoplasms|Biliary Tract Neoplasms|Brain Neoplasm Primary|Carcinoma Ductal Breast|Melanoma|Solid Tumors|Glioblastoma|Bile Duct Neoplasms|Astrocytoma|Head and Neck Squamous Cell Carcinoma|Pontine Glioma|Pancreatic Neoplasms|Ovarian Neoplasms|Carcinoma Renal Cell|Cholangiocarcinoma|Carcinoma|Carcinoma Bronchogenic|Bronchial Neoplasms|Lung Neoplasms|Respiratory Tract Neoplasms|Thoracic Neoplasms|Neoplasms Nerve Tissue|Nevi and Melanomas Loxo Oncology Inc.|Bayer October 2015 Phase 2
NCT02122913 Recruiting Unspecified Adult Solid Tumor Protocol Specific Loxo Oncology Inc.|Bayer May 2014 Phase 1
NCT03025360 Available Cancer|Neurotrophic Tyrosine Kinase Receptor-related Proteins Loxo Oncology Inc.|Bayer null --

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Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID