553008

Raf1 Kinase Inhibitor I

The Raf1 Kinase Inhibitor I, also referenced under CAS 220904-83-6, controls the biological activity of Raf1 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Raf1 Kinase Inhibitor I, 5-Iodo-3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-2-indolinone, GW 5074
• Empirical Formula (Hill Notation): C₁₅H₈Br₂INO₂
• CAS Number: 220904-83-6
• Molecular Weight: 520.94
• MDL number: MFCD03453076
• UNSPSC Code: 12352200
• NACRES: NA.28

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• potency: 9 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: dark orange
• solubility: DMSO: 200 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C15H8Br2INO2/c16-11-4-7(5-12(17)14(11)20)3-10-9-6-8(18)1-2-13(9)19-15(10)21/h1-6,20H,(H,19,21)/b10-3-
• InChI key: LMXYVLFTZRPNRV-KMKOMSMNSA-N

Description

General description

A potent, cell-permeable, reversible, and ATP-competitive cRAF1 kinase inhibitor (IC₅₀ = 9 nM). Shows ≥100-fold selectivity for Raf kinase versus Cdk1, Cdk2, c-Src, ERK2, MEK, p38, Tie2, VEGFR2, and c-Fms. Predicted broad spectrum antitumor agents. A 10 mM (500 µg/96 µl) solution of Raf1 Inhibitor I (Cat. No. 553003) in DMSO is also available.

A potent, cell-permeable, reversible, and ATP-competitive cRaf1 kinase inhibitor (IC₅₀ = 9 nM). Shows ≥100-fold selectivity for Raf kinase versus Cdk1, Cdk2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fms. cRaf1 inhibitors are predicted to be broad spectrum antitumor agents.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
CRAFI kinase

Product competes with ATP.

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.







From Catalog:

Desc. Field- added "Predicted broad spectrum antitumor agents."

Other Notes

Lackey, K., et al. 2000. Bioorg. Med. Chem. Lett.10, 223.

Legal Information

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

Safety Information

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