553018-M

RAF Kinase Inhibitor VII

• Synonym(s): RAF Kinase Inhibitor VII, 1-(4-(2,3-Dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-7-yloxy)-2-(methylthio)phenyl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea
• Empirical Formula (Hill Notation): C₂₁H₁₅ClF₃N₅O₃S
• CAS Number: 884339-61-1
• Molecular Weight: 509.89
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: caramel
• solubility: DMSO: 50 mg/mL
• storage temp.: −20°C

Description

General description

A cell-permeable imidazopyridinyl-urea compound that acts as a potent inhibitor against B-Raf^V600E activity (IC₅₀ = 1 nM) by targeting its ATP-binding pocket and the adjacent lipophilic allosteric site accessible only when the enzyme is in its inactive DFG-out conformation. Reported to effectively inhibit Raf^V600E-dependent ERK phosphorylation (IC₅₀ = 610 nM) and growth of human melanoma WM266.4 cells (GI₅₀ = 470 nM).

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Menard, D., et al. 2009. J. Med. Chem.52, 3881.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable