Sunitinib-d4

CAT: 0804-HY-10255AS1Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-10255AS1Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
[1126721-79-6]
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

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