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658551 AG 1296 - CAS 146535-11-7 - Calbiochem

658551
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
146535-11-7C₁₆H₁₄N₂O₂
Description
OverviewSimilar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC50 = 1.0 µM) and β-receptors (IC50 = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC50 of 300 nM and ~1 µM, respectively.
Catalogue Number658551
Brand Family Calbiochem®
Synonyms6,7-Dimethoxy-3-phenylquinoxaline
References
ReferencesTse, KF., et al. 2002. Leukemia 16, 2027.
Tse, KF., et al. 2001. Leukemia 15, 1001.
Strutz, F., et al. 2001. Kidney Int. 59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.
Product Information
CAS number146535-11-7
ATP CompetitiveY
FormWhite solid
Hill FormulaC₁₆H₁₄N₂O₂
Chemical formulaC₁₆H₁₄N₂O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPDGFR kinase
Primary Target IC<sub>50</sub>1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively
Purity≥98% 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 Standard Handling
Storage -20°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 1 month at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
658551 0

Documentation

AG 1296 - CAS 146535-11-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

AG 1296 - CAS 146535-11-7 - Calbiochem Certificates of Analysis

TitleLot Number
658551

References

Reference overview
Tse, KF., et al. 2002. Leukemia 16, 2027.
Tse, KF., et al. 2001. Leukemia 15, 1001.
Strutz, F., et al. 2001. Kidney Int. 59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.
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.

Revision12-January-2010 RFH
Synonyms6,7-Dimethoxy-3-phenylquinoxaline
DescriptionSimilar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC50 = 1.0 µM) and β-receptors (IC50 = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC50 of 300 nM and ~1 µM, respectively.
FormWhite solid
CAS number146535-11-7
Chemical formulaC₁₆H₁₄N₂O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml) or acetonitrile
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Toxicity Standard Handling
ReferencesTse, KF., et al. 2002. Leukemia 16, 2027.
Tse, KF., et al. 2001. Leukemia 15, 1001.
Strutz, F., et al. 2001. Kidney Int. 59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.