658551 Sigma-AldrichAG 1296 - CAS 146535-11-7 - Calbiochem
A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors and β-receptors.
More>> A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors and β-receptors. Less<<Synonyms: 6,7-Dimethoxy-3-phenylquinoxaline
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Overview
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Key Spec Table
CAS # | Empirical Formula |
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146535-11-7 | C₁₆H₁₄N₂O₂ |
Description | |
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Overview | Similar 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 Number | 658551 |
Brand Family | Calbiochem® |
Synonyms | 6,7-Dimethoxy-3-phenylquinoxaline |
Product Information | |
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CAS number | 146535-11-7 |
ATP Competitive | Y |
Form | White solid |
Hill Formula | C₁₆H₁₄N₂O₂ |
Chemical formula | C₁₆H₁₄N₂O₂ |
Reversible | Y |
Structure formula Image | |
Quality Level | MQ100 |
Applications |
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Biological Information | |
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Primary Target | PDGFR 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 | |
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Cell permeable | Y |
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Safety Information according to GHS |
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Supplemental Information |
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Specifications |
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Global Trade Item Number | |
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Catalogue Number | GTIN |
658551 | 0 |
Documentation
AG 1296 - CAS 146535-11-7 - Calbiochem SDS
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AG 1296 - CAS 146535-11-7 - Calbiochem Certificates of Analysis
Title | Lot Number |
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658551 |
References
Reference overview |
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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 | ||||||||||||||||||||||||||||
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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.
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