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Merck

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

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About This Item

Empirical Formula (Hill Notation):
C20H14ClN3O
CAS Number:
Molecular Weight:
347.80
UNSPSC Code:
12352200
NACRES:
NA.54
MDL number:
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

SMILES string

Clc1c(cc(cc1)c2nc([nH]c2c4ccncc4)c3ccccc3)O

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

General description

A cell-permeable triarylimidazole compound that acts as a reversible, ATP-competitive, and highly potent inhibitor of Raf kinase (IC50 = 10 nM & Kd = 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

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

Disclaimer

Toxicity: Irritant (B)


Storage Class

11 - Combustible Solids

wgk

WGK 3



Certificates of Analysis (COA)

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