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1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine

Base Information Edit
  • Chemical Name:1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine
  • CAS No.:927880-90-8
  • Deprecated CAS:937178-31-9
  • Molecular Formula:C24H16F6N6O
  • Molecular Weight:518.421
  • Hs Code.:
  • UNII:8O434L3768
  • ChEMBL ID:CHEMBL558752
  • DSSTox Substance ID:DTXSID601025871
  • Metabolomics Workbench ID:149607
  • NCI Thesaurus Code:C61311
  • Pharos Ligand ID:3JPLAV8JG919
  • Wikidata:Q27075961
  • Mol file:927880-90-8.mol
1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine

Synonyms:CHIR-265;RAF265

Suppliers and Price of 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine
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
  • TRC
  • RAF265
  • 25mg
  • $ 1260.00
  • Tocris
  • RAF265 ≥98%(HPLC)
  • 10
  • $ 207.00
  • Tocris
  • RAF265 ≥98%(HPLC)
  • 50
  • $ 869.00
  • Medical Isotopes, Inc.
  • RAF265
  • 10 mg
  • $ 740.00
  • Medical Isotopes, Inc.
  • RAF265
  • 25 mg
  • $ 980.00
  • Matrix Scientific
  • 1-Methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]-oxy]-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazol-2-amine 97%
  • 5mg
  • $ 226.00
  • Labseeker
  • RAF265(CHIR-265) 95
  • 1g
  • $ 1692.00
  • DC Chemicals
  • RAF265(CHIR-265) >98%
  • 1 g
  • $ 2100.00
  • DC Chemicals
  • RAF265(CHIR-265) >98%
  • 250 mg
  • $ 1100.00
  • Crysdot
  • RAF265(CHIR-265) 98+%
  • 50mg
  • $ 750.00
Total 57 raw suppliers
Chemical Property of 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine Edit
Chemical Property:
  • Boiling Point:667.6±65.0 °C(Predicted) 
  • PKA:9.07±0.27(Predicted) 
  • PSA:80.65000 
  • Density:1.50 
  • LogP:7.00490 
  • Sensitive.:Light Sensitive 
  • Solubility.:≥25.9 mg/mL in DMSO; insoluble in H2O; ≥7.97 mg/mL in EtOH with ultrasonic 
  • XLogP3:5.4
  • Hydrogen Bond Donor Count:2
  • Hydrogen Bond Acceptor Count:11
  • Rotatable Bond Count:5
  • Exact Mass:518.12897813
  • Heavy Atom Count:37
  • Complexity:763
Purity/Quality:

98%,99%, *data from raw suppliers

RAF265 *data from reagent suppliers

Safty Information:
  • Pictogram(s):  
  • Hazard Codes: 
MSDS Files:

SDS file from LookChem

Useful:
  • Canonical SMILES:CN1C2=C(C=C(C=C2)OC3=CC(=NC=C3)C4=NC=C(N4)C(F)(F)F)N=C1NC5=CC=C(C=C5)C(F)(F)F
  • Recent ClinicalTrials:A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma
  • Recent EU Clinical Trials:A Phase I/II, open-label, dose escalation trial to evaluate the safety, pharmacokinetics, and pharmacodynamics of RAF265 (CHIR-265) administered orally to patients with locally advanced or metastatic melanoma
  • Description RAF265, also known as (CHIR-265), is an arylaminobenzimidazole-based B-RAF, C-RAF, and VEGFR2 inhibitor developed by Chiron Corporation, later acquired by Novartis.
  • Uses RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. RAF 265 is a multikinase inhibitor that has displayed BRAF inhibiting activity in clinical trials. It could be used in the treatment of a subpopulation of human melanoma tumors. Has cytotoxic effect o f on MDA-MB-231 cells. RAF265 when used with BEZ-235 inhibited ERK, PI3K signaling that reduced growth, proliferation and development of drug resistance in human thyroid cancer cells. RAF 265 is a multikinase inhibitor that has displayed BRAF inhibiting activity in clinical trials. It could be used in the treatment of a subpopulation of human melanoma tumors. Has cytotoxic effect of on MDA-MB-231 cells. RAF265 when used with BEZ-235 inhibited ERK, PI3K signaling that reduced growth, proliferation and development of drug resistance in human thyroid cancer cells.
Technology Process of 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine

There total 8 articles about 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine 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:
N1-methyl-4-((2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yl)oxy)benzene-1,2-diamine; 4-(trifluoromethyl)phenyl isothiocyanate; In acetonitrile; at 20 ℃; for 0.333333h;
With 2-chloro-1-methyl-pyridinium iodide; triethylamine; In acetonitrile; at 50 ℃; for 5h; Product distribution / selectivity;
Guidance literature:
4-[1-methyl-2-(4-(trifluoromethyl)phenylamino)-1H-benzoimidazol-5-yloxy]-pyridine-2-carbonitrile; With sodium methylate; In isopropyl alcohol; at 50 ℃; for 1h;
3-bromo-1,1,1-trifluoroacetone; With ammonium acetate; In isopropyl alcohol; at 70 - 85 ℃; for 23h; Product distribution / selectivity;
Guidance literature:
Multi-step reaction with 4 steps
1.1: manganese(IV) oxide / chloroform / 48 h / 20 °C
2.1: sodium acetate / water / 0.67 h / 100 °C
2.2: 20 °C
3.1: palladium 10% on activated carbon; hydrogen / methanol; ethyl acetate / 48 h
4.1: methanol / 16 h / 20 °C
4.2: 20 °C
With manganese(IV) oxide; palladium 10% on activated carbon; hydrogen; sodium acetate; In methanol; chloroform; water; ethyl acetate;
DOI:10.1021/ml500526p
Refernces Edit
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