Apatinib-d8

Apatinib-d8 is intended for use as an internal standard for the quantification of apatinib (Cay-21268) by GC- or LC-MS. Apatinib is a tyrosine kinase inhibitor that potently suppresses the kinase activity of vascular endothelial growth factor 2 (VEGFR2, IC50 = 1 nM). It is less effective against c-Kit (IC50 = 429 nM), RET (IC50 = 13 nM), and c-Src (IC50 = 53 nM) and does not inhibit EGFR, HER2, or FGFR1 (IC50s = >10 µM). Apatinib has been shown to inhibit the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs) stimulated by fetal bovine serum and, either alone or in combination with chemotherapeutic agents, prevents the growth of several established human tumor xenograft models.Formal Name: N-[4-(1-cyanocyclopentyl-2,2,3,3,4,4,5,5-d8)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide. CAS Number: 2468771-43-7. Molecular Formula: C24H15D8N5O. Formula Weight: 405.5. Purity: >99% deuterated forms (d1-d8). Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC=C(C4(C#N)C([2H])([2H])C([2H])([2H])C([2H])([2H])C4([2H])[2H])C=C3. InChi Code: 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. InChi Key: WPEWQEMJFLWMLV-MMBGVTJSSA-N.