Sunitinib malate

Name: Sunitinib malate
Brand: Tocris Bioscience
SKU: 3768

Tocris Bioscience, part of Bio-Techne | Catalog # 3768

Citations (11)

COA / SDS

Potent VEGFR, PDGFRβ and KIT inhibitor

Key Product Details

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)
Molecular Weight:	532.56

View Full Technical Details for Sunitinib malate

Technical Data
Citations

Biological Activity for Sunitinib malate

Sunitinib malate is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (K_i 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 for Sunitinib malate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	1.50 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	1.50 mL

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References for Sunitinib malate

References are publications that support the biological activity of the product.

Roskoski Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem.Biophys.Res.Comm. 2007 PMID: 17367763
O'Farrell SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood 2003 PMID: 12531805
Faivre Molecular basis for suni. efficacy and future clinical development Nat.Rev.Drug Discov. 2007 PMID: 17690708
Mendel 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. 2003 PMID: 12538485