658403

AG 538

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC₅₀ = 400 nM).

• Synonym(s): AG 538, α-Cyano-(3,4-dihydroxy)cinnamoyl-(3ʹ,4ʹ-dihydroxyphenyl)ketone, Tyrphostin AG 538
• Empirical Formula (Hill Notation): C₁₆HN₁₁O₅
• CAS Number: 133550-18-2
• Molecular Weight: 427.25
• MDL number: MFCD00080276
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: dark orange to brown
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1R (insulin-like growth factor-1 receptor) kinase autophosphorylation (IC₅₀ = 400 nM). Also inhibits the phosphorylation of PTK substrate poly (Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC₅₀ = 60 nM, 113 nM, and 2.4 µM respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC₅₀ = 76 µM). Inhibition is competitive with respect to the substrate binding site of IGF-1R kinase. Also inhibits the authophosphorylation of IGF-1R and the activation of PKB and ERK₂ in NIH-3T3 cells over-expressing IGF-1R.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
IGF-1 receptor kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 400 nM against IGF-1 receptor kinase

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

Blum, G., et al. 2000. Biochemistry39, 15705.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable