Nintedanib (free base)

Product description: Chemical. CAS: 656247-17-5. Formula: C31H33N5O4. MW: 539.6. Nintedanib is an orally bioavailable and potent triple angiokinase inhibitor with potential antiangiogenic and antineoplastic activities. It targets the proangiogenic pathways mediated by the the receptor tyrosine kinases VEGFR1/2/3 (IC50=13-34nM), FGFR1/2/3 (IC50=37-108nM) and PDGFRalpha/beta (IC50=59-65nM), 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 competitively binds to the ATP binding-pocket of these receptors, resulting in interference with receptor dimerization and blocking intracellular signaling critical for the proliferation and survival of angiogenesis-related endothelial cells, pericytes and vascular smooth muscle cells. Nintedanib also inhibits some non-receptor kinases such as Fms-like tyrosine protein kinase (Flt-3, IC50=26nM), proto-oncogene ret (Ret, IC50=35nM), lymphocyte-specific tyrosine kinase (Lck, IC50=16nM), tyrosine-protein kinase lyn (Lyn, IC50=195nM) and proto-oncogene tyrosine protein kinase src (Src, IC50=156nM). Through this unique targeting profile nintedanib has significant antitumor activity in several tumor types.

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