Sunitinib malate

Pricing Availability   Qty
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)
Citations (4)
Literature (1)
Pathways (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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.

View Related Products by Product Action

View all VEGFR Inhibitors

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4 Citations for Sunitinib malate

Citations are publications that use Tocris products. Selected citations for Sunitinib malate include:

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

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

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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

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

VEGF Signaling Pathway

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.