IPR-803

IPR-803 is a potent inhibitor of the uPAR·uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity^[1]. IC50 & Target:Ki: 0.2 μM (PPI)^[1] In Vitro: IPR-803 blocks invasion of breast cancer cells line MDA-MB-231, and inhibits matrix metalloproteinase (MMP) breakdown of the extracellular matrix (ECM)^[1].
IPR-803 impairs MDA-MB-231 cell adhesion and migration^[1].
IPR-803 induces a concentration-dependent impairment of cell adhesion with an IC₅₀ of approximately 30 μM^[1].
IPR-803 inhibits MDA-MB-231 cells growth with an IC₅₀ of 58 μM^[1].
IPR-803 (0-200 μM; 3 days) blocks the invasion of MDA-MB-231 cells, and most of the inhibition of cell invasion is unlikely due to cytotoxicity of the compound^[1].
IPR-803 (1-50 μM; 24 hours) does not have a significant effect on apoptosis or necrosis^[1].
IPR-803 (50 μM; 30 minutes) shows inhibition of MAPK phosphorylation^[1].
In Vivo: IPR-803 (200 mg/kg; i.g.; three times a week; for 5 weeks) impairs breast cancer metastasis, but no statistical significance to the differences in body weight between treated and untreated^[1].
IPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue^[1].
IPR-803 exhibits a half-life (t1/2) of 5 hours^[1].