EG 00229 trifluoroacetate

EG00229 is the first small molecule inhibitor of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM(125I-VEGF binding to PAE/NRP1 cells).IC50 value: 8 uM [1]Target: NRP1/VEGF-A inhibitorEG00229 reduced VEGF-A-induced VEGFR2 tyrosine phosphorylation in HUVECs in a dose-dependent fashion, with a maximum inhibition of 34% at 100 μM. EG00229 also significantly reduced VEGF-A induced migration of HUVECs. caused a partial inhibition of VEGF receptor activity and biological function, consistent with the current model for the role of NRP1 in VEGF function, in which NRP1 is required for optimal signaling and certain biological functions downstream of VEGFR2, particularly migration [1].

Research Areas >> Cancer

[1]. Jarvis A, et al. Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J Med Chem. 2010 Mar 11;53(5):2215-26.

[2]. Nissen JC, et al. Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway. J Neurochem. 2013 Nov;127(3):394-402.

Nintedanib (BIBF 1120) | SU5416 | Apatinib Mesylate | PD173074 | Foretinib (GSK1363089) | SU 5402 | Linifanib (ABT-869) | Cediranib | Lucitanib | RAF265 (CHIR-265) | LY2784544 | SU14813 | Dovitinib (TKI-258, CHIR-258) | SAR131675 | Vatalanib (PTK787) 2HCl