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121850 AGL 2263

121850
  
Purchase on Sigma-Aldrich

Overview

Replacement Information
Description
Overview

This product has been discontinued.

We apologize for the inconvenience, but we do not currently have an alternative product. Please refer to our complete listing of receptor tyrosine kinase inhibitors for possible alternatives. Please read the alternative product documentation carefully and contact technical service if you need additional information.





A cell-permeable benzoxazolone-containing bioisostere of tyrphostin AG 538 (Cat. No. 658403) that acts as a potent, substrate-competitive, but not ATP-competitive, inhibitor of insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R). It is selective towards IR and IGF-1R (IC50 = 0.4 and 0.43 µM, respectively) and inhibits Src and PKB only at much higher concentrations (IC50 = 2.2 and 55 µM, respectively) in kinase assays. Shown to prevent IGF-1-induced cellular IGF-1R autophosphorylation and down stream signalling. Specifically inhibits IGF-1-induced, but not PDGF-induced, activation of PKB in cells. Effectively blocks the formation of colonies in soft agar by breast and prostate cancer cells. Exhibits improved cellular oxidative stability than AG 538.
Catalogue Number121850
Brand Family Calbiochem®
SynonymsAG 2263
References
ReferencesBlum, G., et al. 2003. J. Biol. Chem. 278, 40442.
Product Information
ATP CompetitiveY
FormYellow solid
Hill FormulaC₁₇H₁₀N₂O₅
Chemical formulaC₁₇H₁₀N₂O₅
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetIGF-1R
Primary Target IC<sub>50</sub>0.43 µM
Secondary targetIR (IC₅₀ = 0.4 µM) and inhibits Src and PKB at (IC₅₀ = 2.2 and 55 µM, respectively)
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Carcinogenic / Teratogenic
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

AGL 2263 Certificates of Analysis

TitleLot Number
121850

References

Reference overview
Blum, G., et al. 2003. J. Biol. Chem. 278, 40442.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision08-April-2008 RFH
SynonymsAG 2263
DescriptionA cell-permeable, bioisostere of AG 538 (Cat. No. 658403) that acts as a potent, substrate-competitive inhibitor of insulin receptor (IR) tyrosine kinase (IC50 = 400 nM) and insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase (IC50 = 430 nM). Inhibits Src and protein kinase B (PKB/Akt) activities only at higher concentrations (IC50 = 2.2 µM and 55 µM, respectively). Reported to block IGF-1-induced cellular IGF-1R autophosphorylation and downstream signaling. Also reported to specifically inhibit IGF-1-induced, but not PDGF-induced, PKB activation in cells. Shown to effectively block the formation of breast cancer cell and prostate cancer cell colonies in soft agar. Exhibits much improved cellular oxidative stability compared to AG 538.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₇H₁₀N₂O₅
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Carcinogenic / Teratogenic
ReferencesBlum, G., et al. 2003. J. Biol. Chem. 278, 40442.