Pazopanib-13C,d3 hydrochloride

Names

[ CAS No. ]:
1261398-44-0

[ Name ]:
Pazopanib-13C,d3 hydrochloride

[Synonym ]:
Benzenesulfonamide, 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methyl-13C-d3-amino]-2-pyrimidinyl]amino]-2-methyl-, hydrochloride (1:1)
5-[(4-{(2,3-Dimethyl-2H-indazol-6-yl)[(13C,2H3)methyl]amino}-2-pyrimidinyl)amino]-2-methylbenzenesulfonamide hydrochloride (1:1)

Biological Activity

[Description]:

Pazopanib-13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

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

[2]. Harris PA, et al. Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem. 2008, 51(15), 4632-4640.  

[3]. Thakur A, et al. Pazopanib, a multitargeted tyrosine kinase inhibitor, reduces diabetic retinal vascular leukostasis and leakage. Microvasc Res. 2011 Nov82(3):346-50.  

Chemical & Physical Properties

[ Molecular Formula ]:
C2013CH21D3ClN7O2S

[ Molecular Weight ]:
477.990

[ Exact Mass ]:
477.162262

Related Compounds