NRPa-308 is a small molecule neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.
NRPa-308 exhibits cellular activity with IC50 of 0.5 uM on a human aggressive and metastatic estrogenR−/progesteroneR−/Her2- breast cancer cell line (MDA-MB-231).
NRPa-308 dramatically inhibits tubulogenesis for HUVEC tubule formation in a collagen gel under VEGF-A165 stimulation.
NRPa-308 (50 mg/kg) improves the median survival and reduces the tumour growth on mice xenografted with human breast cancer cells (MDA-MB-231), does not exert visible acute toxicity.
