IPR-803

Modify Date: 2023-01-14 17:05:04

IPR-803 Structure
IPR-803 structure
 Common Name IPR-803
CAS Number 892243-35-5 Molecular Weight 453.49
Density N/A Boiling Point N/A
Molecular Formula C27H23N3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name IPR-803

 IPR-803 Biological Activity

Description 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].
Related Catalog
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]. Cell Proliferation Assay[1] Cell 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 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]. Animal Model: NSG mice with MDA-MB-231 cells xenograft[1] 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[1] Dosage: 200 mg/kg (Pharmacokinetic Study) Administration: Oral administration Result: t1/2=5 hours.
References

[1]. Mani T, et al. Small-molecule inhibition of the uPAR•uPA interaction: synthesis, biochemical, cellular, in vivo pharmacokinetics and efficacy studies in breast cancer metastasis. Bioorg Med Chem. 2013 Apr 1;21(7):2145-55.

 Chemical & Physical Properties

Molecular Formula C27H23N3O4
Molecular Weight 453.49
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Chemsrc provides IPR-803(CAS#:892243-35-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of IPR-803 are included as well.>> amp version: IPR-803

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