553014

Raf Kinase Inhibitor IV

The Raf Kinase Inhibitor IV, also referenced under CAS 303727-31-3, controls the biological activity of Raf Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Raf Kinase Inhibitor IV, 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole, L 779450
• Empirical Formula (Hill Notation): C₂₀H₁₄ClN₃O
• CAS Number: 303727-31-3
• Molecular Weight: 347.80
• MDL number: MFCD12828750
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• potency: 10 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: ethanol: 10 mg/mL; DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C20H14ClN3O/c21-16-7-6-15(12-17(16)25)19-18(13-8-10-22-11-9-13)23-20(24-19)14-4-2-1-3-5-14/h1-12,25H,(H,23,24)
• InChI key: WXJLXRNWMLWVFB-UHFFFAOYSA-N

Description

General description

A cell-permeable triarylimidazole compound that acts as a reversible, ATP-competitive, and highly potent inhibitor of Raf kinase (IC₅₀ = 10 nM & K_d = 2.4 nM for B-raf) with 7-, 30-, and 70-fold selectivity over p38α, GSK-3β, and Lck, respectively. Cellular data have indicated that the compound is more effective towards Raf-1and A-Raf than B-Raf.

A cell-permeable triarylimidazole compound that acts as a reversible, ATP-competitive, and highly potent inhibitor of Raf kinase (IC₅₀ = 10 nM and K_d = 2.4 nM for B-raf) with 7-, 30-, and 70-fold selectivity over p38α, GSK-3β, and Lck, respectively. Cellular data have indicated that the compound is more effective towards Raf-1and A-Raf than B-Raf.

Biochem/physiol Actions

Cell permeable: yes

Kd = 2.4 nM for B-raf

Primary Target
Raf Kinase

Product competes with ATP.

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Other Notes

Takle, A.K., et al. 2006. Bioorg. Med. Chem. Lett.16, 378.
Shelton, J.G., et al. 2003. Leukemia17, 1765.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3