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Submit ReviewSunitinib malate
Description: Potent VEGFR, PDGFRβ and KIT inhibitor
Alternative Names: SU 11248
Chemical Name: N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-2-hydroxybutanedioate salt
Purity: ≥99% (HPLC)
Biological Activity for Sunitinib malate
Sunitinib malate is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for Sunitinib malate
Sunitinib malate is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Sunitinib malate
| M. Wt | 532.56 |
| Formula | C22H27FN4O2.C4H6O5 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 341031-54-7 |
| PubChem ID | 6456015 |
| InChI Key | LBWFXVZLPYTWQI-IPOVEDGCSA-N |
| Smiles | O=C(NCCN(CC)CC)C1=C(C)NC(/C=C2\C(NC3=C2C=C(F)C=C3)=O)=C1C.OC(C[C@H](O)C(O)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Sunitinib malate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.31 | 25 |
Preparing Stock Solutions for Sunitinib malate
The following data is based on the product molecular weight 532.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 7.51 mL | 37.55 mL | 75.11 mL |
| 1.25 mM | 1.5 mL | 7.51 mL | 15.02 mL |
| 2.5 mM | 0.75 mL | 3.76 mL | 7.51 mL |
| 12.5 mM | 0.15 mL | 0.75 mL | 1.5 mL |
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Product Datasheets for Sunitinib malate
References for Sunitinib malate
References are publications that support the biological activity of the product.
Mendel et al (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. Clin.Cancer Res. 9 327 PMID: 12538485
O'Farrell et al (2003) SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood 101 3597 PMID: 12531805
Faivre et al (2007) Molecular basis for suni. efficacy and future clinical development Nat.Rev.Drug Discov. 6 734 PMID: 17690708
Roskoski (2007) Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem.Biophys.Res.Comm. 356 323 PMID: 17367763
If you know of a relevant reference for Sunitinib malate, please let us know.
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Keywords: Sunitinib malate, Sunitinib malate supplier, Potent, VEGFR, PDGRb, PDGFRbeta, PDGFRβ, FGFR, inhibitors, inhibits, Vascular, Endothelial, Growth, Factor, Receptors, KDR, Flt, Flk, Kit, Receptor, Tyrosine, Kinases, RTKs, Fibroblast, platelet, derived, CD117, SU11248, Pfizer, SU, 11248, PDGFR, Other, 3768, Tocris Bioscience
4 Citations for Sunitinib malate
Citations are publications that use Tocris products. Selected citations for Sunitinib malate include:
Procaccia et al (2014) Gleevec/imatinib, an ABL2 kinase inhibitor, protects tumor and endothelial cells from semaphorin-induced cytoskeleton collapse and loss of cell motility. Biochem Biophys Res Commun 448 134 PMID: 24759231
Goel et al (2014) VEGF???-conjugated mesoporous silica nanoparticle: a tumor targeted drug delivery system. ACS Appl Mater Interfaces 6 21677 PMID: 25353068
Gaji et al (2014) Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother 58 2598 PMID: 24550330
Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Cell Death Differ 8 ra42 PMID: 25943352
Do you know of a great paper that uses Sunitinib malate from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Pathways for Sunitinib malate
