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Merck
CN

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:
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Product Name

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.

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

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

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Kd = 2.4 nM for B-raf
Primary Target
Raf Kinase
Product competes with ATP.
Reversible: yes

Disclaimer

Toxicity: Irritant (B)

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.

Other Notes

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

Packaging

Packaged under inert gas

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Related Content

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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