Sunitinib (Malate)
Sunitinib (SU 11248) Malat is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib Malat, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
Product Specifications
CAS Number
[341031-54-7]
Product Name Alternative
SU 11248 (Malate)
UNSPSC
12352005
Hazard Statement
H360, H372
Target
Apoptosis; Autophagy; IRE1; Mitophagy; PDGFR; VEGFR
Type
Reference compound
Related Pathways
Apoptosis; Autophagy; Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer; Infection; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/Sunitinib-Malate.html
Concentration
10mM
Purity
99.61
Solubility
DMSO : ≥ 15 mg/mL|H2O : 12.5 mg/mL (ultrasonic; adjust pH to 3 with HCl) |H2O : 3.33 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C(NCCN(CC)CC)C1=C(NC(/C=C2C(NC3=C\2C=C(C=C3)F)=O)=C1C)C.O=C([C@H](CC(O)=O)O)O
Molecular Formula
C26H33FN4O7
Molecular Weight
532.56
Precautions
H360, H372
References & Citations
[1]Sun L, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol- (3Z) -ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl) amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor r|[2]Ali MM, et al. Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response. EMBO J. 2011 Mar 2;30 (5) :894-905.|[3]O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101 (9) :3597-605.|[4]Mendel DB, et al. 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 Can
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PDGFRβ; VEGFR2/KDR/Flk-1
Citation 01
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