Sunitinib malate

Pricing Availability Delivery Time Qty
Cat.No. 3768 - Sunitinib malate | C22H27FN4O2.C4H6O5 | CAS No. 341031-54-7
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)
Datasheet
Citations (2)
Literature
Pathways

Biological Activity

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

Sunitinib malate is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox I and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 13.31 25

Preparing Stock Solutions

The following data is based on the product molecular weight 532.56. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 1.88 mL 9.39 mL 18.78 mL
5 mM 0.38 mL 1.88 mL 3.76 mL
10 mM 0.19 mL 0.94 mL 1.88 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 sunitinib 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:


If you know of a relevant reference for Sunitinib malate, please let us know.

View Related Products by Product Action

View all VEGFR Inhibitors

Keywords: 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 VEGFR

2 Citations for Sunitinib malate

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

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


Do you know of a great paper that uses Sunitinib malate from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Sunitinib malate

VEGF

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.

Protocols

TODO: Add Protocols