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 11 publications
3 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.
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)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
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.
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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.