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Sunitinib D10

Names

[ CAS No. ]:
1126721-82-1

[ Name ]:
Sunitinib D10

[Synonym ]:
Sunitinib-d10
Sutent-d10

Biological Activity

[Description]:

Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib 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].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Cell Cycle/DNA Damage >> IRE1
Signaling Pathways >> Autophagy >> Mitophagy
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

[Target]

VEGFR2:80 nM (IC50)

PDGFRβ:2 nM (IC50)


[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H17D10FN4O2

[ Molecular Weight ]:
408.53500

[ Exact Mass ]:
408.27500

[ PSA ]:
84.21000

[ LogP ]:
3.99480

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds