IPR-803 (C09-1140-379)

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 activityIn VitroIPR-803 blocks invasion of breast cancer cells line MDA-MB-231, and inhibits matrix metalloproteinase (MMP) breakdown of the extracellular matrix (ECM). ?/nIPR-803 impairs MDA-MB-231 cell adhesion and migration. ?/nIPR-803 induces a concentration-dependent impairment of cell adhesion with an IC 50 of approximately 30 μM. ?/nIPR-803 inhibits MDA-MB-231 cells growth with an IC 50 of 58 μM. ?/nIPR-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. ?/nIPR-803 (1-50 μM; 24 hours) does not have a significant effect on apoptosis or necrosis. ?/nIPR-803 (50 μM; 30 minutes) shows inhibition of MAPK phosphorylation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: MDA-MB-231 cells Concentration: 0 μM, 50 μM, 150 μM, 200 μM Incubation Time: 3 days Result: Displays 90 percent blockage of invasion that is observed at 50 μM.In VivoIPR-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 . ?/nIPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue . ?/nIPR-803 exhibits a half-life (t1/2) of 5 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NSG mice with MDA-MB-231 cells xenograft Dosage: 200 mg/kg Administration: Oral gavage; three times a week; for 5 weeks Result: Impaired metastasis to the lungs. Animal Model: NOD/SCID mice Dosage: 200 mg/kg (Pharmacokinetic Study) Administration: Oral administration Result: t1/2=5 hours.Form:SolidIC50& Target:Ki: 0.2 μM (PPI). Specification: ≥98.0% Molecular Formula: C27H23N3O4 Molecular Weight: 453.49 PubChem CID: 3675673 Isomeric SMILES: C1CCCN(CC1)C2=CC(=C3C4=C(C5=CC=CC=C5C3=O)ON=C24)NC6=CC=CC(=C6)C(=O)O