Formulation: A solid
Formal Name: N-[4-(1-cyanocyclopentyl-2,2,3,3,4,4,5,5-d8)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide
Purity: ≥99% deuterated forms (d1-d8)
Formula Markup: C24H15D8N5O
Formula Weight: 405,5
Shelf life (days): 1460
CAS Number: 2468771-43-7
Notes: Apatinib-d8 is intended for use as an internal standard for the quantification of apatinib (Item No. 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).{33574} 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).{33574} 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.{33574}
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