Sunitinib (glucuronate)

Sunitinib (SU 11248) glucuronate is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib glucuronate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

Product Specifications

CAS Number

[1818285-48-1]

Product Name Alternative

SU 11248 (glucuronate)

UNSPSC

12352005

Target

Apoptosis; Autophagy; IRE1; Mitophagy; PDGFR; VEGFR

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Purity

95.0

Smiles

O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C(O)=O.O=C(/C(C1=C2)=C\C3=C(C(C(NCCN(CC)CC)=O)=C(N3)C)C)NC1=CC=C2F

Molecular Formula

C28H37FN4O9

Molecular Weight

592.61

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 receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46 (7) :1116-9.|[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, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM. 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 Jan;9 (1) :327-37.