Larotrectinib (LOXO-101) sulfate
Catalog No.S7960 Synonyms: ARRY-470, Larotrectinib
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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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.
Purity & Quality Control
Choose Selective Trk receptor Inhibitors
|Description||Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).|
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.
|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.|
|In vitro||DMSO||100 mg/mL (189.92 mM)|
|Ethanol||100 mg/mL (189.92 mM)|
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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|
|NCT03155620||Recruiting||Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|Childhood Langerhans Cell Histiocytosis|Histiocytic Sarcoma|Juvenile Xanthogranuloma|Malignant Glioma|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|Recurrent Rhabdoid Tumor|Refractory Central Nervous System Neoplasm|Refractory Childhood Malignant Germ Cell Tumor|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|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|
|NCT02465060||Recruiting||Advanced Malignant Solid Neoplasm|Bladder Carcinoma|Breast Carcinoma|Cervical Carcinoma|Colon Carcinoma|Colorectal Carcinoma|Endometrial Carcinoma|Esophageal Carcinoma|Gastric Carcinoma|Glioma|Head and Neck Carcinoma|Kidney Carcinoma|Liver and Intrahepatic Bile Duct Carcinoma|Lung Carcinoma|Lymphoma|Malignant Uterine Neoplasm|Melanoma|Ovarian Carcinoma|Pancreatic Carcinoma|Plasma Cell Myeloma|Prostate Carcinoma|Rectal Carcinoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Cervical Carcinoma|Recurrent Colon Carcinoma|Recurrent Colorectal Carcinoma|Recurrent Esophageal Carcinoma|Recurrent Gastric Carcinoma|Recurrent Glioma|Recurrent Head and Neck Carcinoma|Recurrent Liver Carcinoma|Recurrent Lung Carcinoma|Recurrent Lymphoma|Recurrent Malignant Solid Neoplasm|Recurrent Melanoma|Recurrent Ovarian Carcinoma|Recurrent Pancreatic Carcinoma|Recurrent Plasma Cell Myeloma|Recurrent Prostate Carcinoma|Recurrent Rectal Carcinoma|Recurrent Skin Carcinoma|Recurrent Thyroid Gland Carcinoma|Recurrent Uterine Corpus Carcinoma|Refractory Lymphoma|Refractory Malignant Solid Neoplasm|Refractory Plasma Cell Myeloma|Skin Carcinoma|Thyroid Gland Carcinoma|Uterine Corpus Cancer||National Cancer Institute (NCI)||August 12 2015||Phase 2|
|NCT02122913||Recruiting||Unspecified Adult Solid Tumor Protocol Specific||Loxo Oncology Inc.|Bayer||May 2014||Phase 1|
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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