Nintedanib esylate

Description: Nintedanib esylate (formerly also known as BIBF 1120 esylate; trade name: Vargatef) is a novel, orally bioavailable, potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRalpha/beta with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Intedanib selectively binds to and inhibits VEGFR, FGFR and PDGFR)tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. Nintedanib was approved by FDA for the treatment of idiopathic pulmonary fibrosis (IPF) on Nov 15, 2014.

References: Cancer Res. 2008 Jun 15; 68(12):4774-82; J Med Chem. 2009 Jul 23; 52(14):4466-80.

Related CAS: 928326-83-4 (free base); 656247-18-6 (esylate); 656247-17-5 (free base)