Sunitinib . malate
AG-CR1-3707-M0011 mgCHF 40.00
AG-CR1-3707-M0055 mgCHF 70.00
AG-CR1-3707-M02525 mgCHF 120.00
AG-CR1-3707-M500500 mgCHF 325.00
C22H27FN4O2 . C4H6O5
|MW||398.5 . 134.1|
|Solubility||Soluble in DMSO (10mg/ml) or ethanol.|
|Identity||Determined by 1H-NMR.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent ATP-competitive and cell permeable multi-targeted receptor tyrosine kinase (RTK) inhibitor targeting VEGFR and PDGFR-β. Inhibits FLK1 (Ki=9nM), PDGFRβ (Ki=8nM) and FLT3. It is at least 10-fold selective for FLK1 and PDGFRβ over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl and Src.
- Inhibits the cellular receptor phosphorylation of FLT3, RET and CSF-1R.
- Also shown to inhibit c-Kit.
- Exhibits potent antiangiogenic and antitumor activity in multiple xenograft models.
- Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase: L. Sun, et al.; J. Med. Chem. 46, 1116 (2003)
- In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship: D. B. Mendel, et al.; Clin. Cancer Res. 9, 327 (2003)
- SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo: A.M. O'Farrell, et al.; Blood 101, 3597 (2003)
- Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors: J. Guo, et al.; Mol. Cancer. Ther. 5, 1007 (2006)
- Molecular basis for sunitinib efficacy and future clinical development: S. Faivre, et al.; Nat. Rev. Drug Discov. 6, 734 (2007)
- Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor: R. Roskoski; BBRC 356, 323 (2007)