Sunitinib-d4

• Description:

  Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

• UNSPSC:

  12352005

• Target:

  Apoptosis; Autophagy; IRE1; Isotope-Labeled Compounds; Mitophagy; PDGFR; VEGFR

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

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

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Solubility:

  10 mM in DMSO

• Smiles:

  C(=C\1/C=2C(NC1=O)=CC=C(F)C2)\C3=C(C)C(C(NC(C(N(CC)CC)([2H])[2H])([2H])[2H])=O)=C(C)N3

• Molecular Formula:

  C22H23D4FN4O2

• Molecular Weight:

  402.50

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.|[4]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.|[5]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

• Scientific Category:

  Isotope-Labeled Compounds

• Clinical Information:

  No Development Reported

• CAS Number:

  1126721-79-6