WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205916
Description: PF-00337210 is an orally available ATP-competitive inhibitor of the vascular endothelial growth factor receptor type 2 (VEGFR2), with potential anti-angiogenesis and antineoplastic activities. Upon administration, the VEGFR2 tyrosine kinase inhibitor PF-00337210 selectively binds to VEGFR2 and prevents its phosphorylation which may result in an inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and may eventually cause tumor cell death. VEGFR2, a receptor tyrosine kinase, is frequently overexpressed by a variety of tumor types.
MedKoo Cat#: 205916
Chemical Formula: C26H27N3O5
Exact Mass: 461.19507
Molecular Weight: 461.51
Elemental Analysis: C, 67.66; H, 5.90; N, 9.10; O, 17.33
Synonym: PF00337210; PF 00337210; PF-00337210; P337210; PF-337210; PF337210.
IUPAC/Chemical Name: N,2-dimethyl-6-((7-(2-morpholinoethoxy)quinolin-4-yl)oxy)benzofuran-3-carboxamide
InChi Key: LGXVKMDGSIWEHL-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H27N3O5/c1-17-25(26(30)27-2)21-6-4-19(16-24(21)33-17)34-23-7-8-28-22-15-18(3-5-20(22)23)32-14-11-29-9-12-31-13-10-29/h3-8,15-16H,9-14H2,1-2H3,(H,27,30)
SMILES Code: O=C(C1=C(C)OC2=CC(OC3=CC=NC4=CC(OCCN5CCOCC5)=CC=C34)=CC=C12)NC
PF-00337210 is a highly potent and selective ATP-competitive inhibitor of VEGFR2 TK with a cellular IC50 of 0.8 nM. In vivo, it inhibits tumor angiogenesis and human xenograft growth. Modulation of blood pressure (BP) and vascular permeability (volume transfer constant: Ktrans) appear to be suitable markers of efficacy for VEGF/VEGFR inhibitors. PF-00337210 is well tolerated at 6 mg BID, with profound VEGFR inhibition effects (as measured by elevated BP and a significant decrease in tumor vascular parameters by DCE-MRI). (source: http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=74&abstractID=50129).
1: Marra MT, Khamphavong P, Wisniecki P, Gukasyan HJ, Sueda K. Solution formulation development of a VEGF inhibitor for intravitreal injection. AAPS PharmSciTech. 2011 Mar;12(1):362-71. Epub 2011 Feb 11. PubMed PMID: 21312012; PubMed Central PMCID: PMC3066352.