Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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R127906-1mg | 1mg | In stock | $27.90 | |
R127906-5mg | 5mg | In stock | $113.90 | |
R127906-10mg | 10mg | In stock | $195.90 | |
R127906-50mg | 50mg | In stock | $608.90 |
Raf kinase and VEGFR-2 inhibitor
Synonyms | RAF265 | 927880-90-8 | CHIR-265 | RAF-265 | RAF 265 | RAF265(CHIR-265) | RAF265 (CHIR-265) | CHIR 265 | 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine | 1-Methyl-5-[[2-[5-(trifluoromethyl)-1h-imidazol- |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Raf kinase and VEGFR-2 inhibitor. Inhibits c-Raf, wild type B-Raf and mutant B-Raf (V600E). Cytotoxic in certain melanoma cells lines. Effects enhanced by protein kinase D3 inhibition, preventing reactivation of MAPK signaling and increasing caspase activ |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Vascular endothelial growth factor receptor 2 inhibitor |
Product Description | RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2. |
ALogP | 5.4 |
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Pubchem Sid | 488197644 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488197644 |
IUPAC Name | 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine |
INCHI | InChI=1S/C24H16F6N6O/c1-36-19-7-6-15(10-17(19)34-22(36)33-14-4-2-13(3-5-14)23(25,26)27)37-16-8-9-31-18(11-16)21-32-12-20(35-21)24(28,29)30/h2-12H,1H3,(H,32,35)(H,33,34) |
InChi Key | YABJJWZLRMPFSI-UHFFFAOYSA-N |
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 |
Isomeric 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 |
PubChem CID | 11656518 |
Molecular Weight | 518.43 |
CAS Registry No. | 927880-90-8 |
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DiscoveRx TREEspot | A-674563|CHIR-265/RAF-265| |
PubChem CID | 11656518 |
ChEMBL Ligand | CHEMBL558752 |
RCSB PDB Ligand | 55J |
PubChem SID | 488197644 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
D2319056 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319057 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319058 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319060 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319061 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319063 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319064 | Certificate of Analysis | Mar 15, 2023 | R127906 |
D2319065 | Certificate of Analysis | Mar 15, 2023 | R127906 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 51.84, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 10.37, Max Conc. mM: 20 |
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1. Mordant P, Loriot Y, Leteur C, Calderaro J, Bourhis J, Wislez M, Soria JC, Deutsch E. (2010) Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination.. Mol Cancer Ther, 9 (2): (358-68). [PMID:20124452] |