Cabozantinib-d4

Names

[ CAS No. ]:
1802168-53-1

[ Name ]:
Cabozantinib-d4

Biological Activity

[Description]:

Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> TAM Receptor
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR

[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;53(2):211-216.

[2]. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768.

[3]. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308.

[4]. Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H20D4FN3O5

[ Molecular Weight ]:
505.53

Related Compounds