Larotrectinib (LOXO-101) sulfate
For research use only.
Catalog No.S7960 Synonyms: ARRY-470, Larotrectinib
CAS No. 1223405-08-0
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.
Selleck's Larotrectinib (LOXO-101) sulfate has been cited by 10 publications
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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.
Immunoblot analysis for FRS2, AKT, and ERK activity for NCI-H2077 cells treated for 48 hours with DMSO, BGJ398, or additional kinase inhibitors as indicated, or combination treatment as indicated (Tram, trametinib; LDC, LDC1267; LOXO, LOXO-101; Imat, imatinib; MGCD, MGCG-265).
Mol Cancer Ther, 2018, 17(7):1526-1539. 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 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.|
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)|
* 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.
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，)
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.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04655404||Not yet recruiting||Drug: Larotrectinib|Procedure: Larotrectinib||High Grade Glioma||Nationwide Children''s Hospital||February 1 2021||Early Phase 1|
|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 (Vitravki 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|
|NCT02122913||Active not recruiting||Drug: Larotrectinib (Vitrakvi BAY2757556)||Solid Tumors Harboring NTRK Fusion||Bayer||May 4 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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