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LOXO-101

Base Information Edit
LOXO-101

Synonyms:LOXO-101;(R)-N-(5-((S)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide;(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide;ARRY 470;Larotrectinib

Suppliers and Price of LOXO-101
Supply Marketing:Edit
Business phase:
The product has achieved commercial mass production*data from LookChem market partment
Manufacturers and distributors:
  • Manufacture/Brand
  • Chemicals and raw materials
  • Packaging
  • price
  • Usbiological
  • Larotrectinib
  • 5mg
  • $ 460.00
  • TRC
  • Larotrectinib
  • 5mg
  • $ 75.00
  • DC Chemicals
  • Larotrectinib(LOXO-101freebase) >98%
  • 100 mg
  • $ 450.00
  • DC Chemicals
  • Larotrectinib(LOXO-101freebase) >98%
  • 1 g
  • $ 1300.00
  • DC Chemicals
  • Larotrectinib(LOXO-101freebase) >98%
  • 250 mg
  • $ 700.00
  • Crysdot
  • LOXO-101 98+%
  • 10mg
  • $ 644.00
  • ChemScene
  • Larotrectinib 99.93%
  • 100mg
  • $ 840.00
  • ChemScene
  • Larotrectinib 99.93%
  • 5mg
  • $ 84.00
  • ChemScene
  • Larotrectinib 99.93%
  • 10mg
  • $ 144.00
  • ChemScene
  • Larotrectinib 99.93%
  • 50mg
  • $ 504.00
Total 74 raw suppliers
Chemical Property of LOXO-101 Edit
Chemical Property:
  • Appearance/Colour:White to yellow solid 
  • PKA:8.41±0.40(Predicted) 
  • PSA:86.00000 
  • Density:1.55±0.1 g/cm3(Predicted) 
  • LogP:3.02340 
  • Storage Temp.:RT 
  • Solubility.:Soluble in DMSO (up to 5 mg/ml). 
Purity/Quality:

98%min *data from raw suppliers

Larotrectinib *data from reagent suppliers

Safty Information:
  • Pictogram(s):  
  • Hazard Codes: 
MSDS Files:
Useful:
  • Description Larotrectinib (VITRAKVIR) is an orally administered, small molecule, highly-selective, tropomyosin receptor kinase (TRK) inhibitor that was developed by Loxo Oncology in collaboration with Bayer AG as a treatment for adult and paediatric patients whose cancers harbour neurotrophic receptor tyrosine kinase (NTRK) gene fusions.? Larotrectinib is a highly selective, potent inhibitor of TRKA, TRKB and TRKC (in vitro 50% inhibitory constant 5–11 nmol/L), with minimal or no activity against other kinase and non-kinase targets [1, 2]. Inhibition of TRKs prevents TRK activation, resulting in both the induction of cellular apoptosis and the inhibition of cell growth in tumours that overexpress TRKs. LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 μM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = <100, <10, and <10 nM, respectively). In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
  • Uses LOXO-101 is a drug used to treat adults and children with certain types of solid tumors that have spread or cannot be removed by surgery and have the?NTRK?gene fusion. It is also being studied in the treatment of other types of cancer. Larotrectinib is a TRK Inhibitor (Tyrosine kinase inhibitor).
Technology Process of LOXO-101

There total 17 articles about LOXO-101 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:
Guidance literature:
With zinc(II) tetrahydroborate; In 2-methyltetrahydrofuran; at 50 - 60 ℃; for 3h; Solvent; Reagent/catalyst;
Guidance literature:
5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-amine; 1,1'-carbonyldiimidazole; In dichloromethane; at 20 ℃; for 2h;
3-hydroxypyrrolidine; In dichloromethane; for 0.0833333h;
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