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Sunitinib malate

Catalog No.
A8255
VEGFR/PDGFRβ/ KIT/ FLT3/RET/CSF-1R inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
Evaluation Sample
$30.00
In stock
100mg
$50.00
In stock
500mg
$100.00
In stock
1g
$150.00
In stock
2g
$200.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Sunitinib malate (CAS 341031-54-7) is a small molecule, orally bioavailable multitargeted receptor tyrosine kinase inhibitor. It inhibits various receptor tyrosine kinases, including platelet-derived growth factor receptor (PDGFR), vascular endothelial growth factor receptors (VEGFR-1, 2, and 3), c-KIT, FLT3 kinase, colony-stimulating factor-1 receptor (CSF-1R), and RET kinase. In neuroblastoma cell lines (e.g., SK-N-BE(2), SH-SY5Y, LAN-5), treatment with sunitinib malate significantly suppresses proliferation in a dose-dependent manner (IC50 ~10-20 ng/ml). Preclinical studies show tumor growth inhibition and reduced metastasis in neuroblastoma mouse models, highlighting its potential for research in oncology therapeutics.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at 4°C
M.Wt532.56
Cas No.341031-54-7
FormulaC22H27FN4O2·C4H6O5
SynonymsSU 11248,SU11248,SU-11248,Sunitinib
Solubility≥26.65 mg/mL in DMSO; insoluble in EtOH; ≥4.6 mg/mL in H2O with ultrasonic
Chemical NameN-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide;(2S)-2-hydroxybutanedioic acid
SDFDownload SDF
Canonical SMILESCCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

NIH-3T3 cells, HUVECs

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Applications

In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibited VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation. Sunitinib inhibited VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively.

Animal experiment [1]:

Animal models

Tumor xenograft mouse models bearing HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435 cells

Dosage form

Oral dosing, 20-80 mg/kg/day, once daily

Application

Sunitinib (20-80 mg/kg/day) exhibited broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib (80 mg/kg/day for 21 days) led to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Sunitinib treatment significantly decreased tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 completely inhibited additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Mendel D B, Laird A D, Xin X, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors[J]. Clinical Cancer Research, 2003, 9(1): 327-337.

Biological Activity

Description Sunitinib Malate is a multi-targeted inhibitor of RTK for VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM.
Targets VEGFR2 (Flk-1) PDGFRβ        
IC50 80 nM 2 nM        

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