Apatinib-d8

CAS: 811803-05-1

Ref. TR-A726153

Product Information

• Name: Apatinib-d8
• Synonyms: 3-Pyridinecarboxamide, N-[4-(1-cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-, Apatinib, Apatinib (YN968D1), Apatinib mesylate, Aptinib, N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide, N-[4-(1-cyanocyclopentyl)phenyl]-2-[(pyridin-4-ylmethyl)amino]pyridine-3-carboxamide, Rivoceranib, Yn 968D1, N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]pyridine-3-carboxamide

Description

Applications Apatinib-d8 is an intermediate used in the synthesis of Apatinib-d8 Hydrochloride (A726152), which is a labelled Apatinib (A726150). Apatinib is an orally available, small molecule multitargeted tyrosine kinase inhibitor. Apatinib selectively inhibits the vascular endothelial growth factor receptor-2 (VEGFR2). Apatinib functions by inhibiting VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. Recent studies have shown that Apatinib enhances the efficacy of conventional chemotherapeutical drugs in side population (SP) cells and ABCB1-overexpressing leukemia cells.
References Mi, Y. et al.: Cancer Res., 70, 7981 (2010); Tong, X.Z. et al.: Biochem. Pharmacol., 83, 586 (2012); Ding, J, et al.: J. Chrom B Anal. Technol. Biomed. Life Sci., 895, 108 (2012);

• Brand: TRC

Chemical properties

• Molecular weight: 405.53
• Formula: C₂₄H₁₅D₈N₅O
• Color/Form: Neat
• InChI: InChI=1S/C24H23N5O/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30)/i1D2,2D2,11D2,12D2
• SMILES: [2H]C1([2H])C([2H])([2H])C([2H])([2H])C(C#N)(c2ccc(NC(=O)c3cccnc3NCc3ccncc3)cc2)C1([2H])[2H]