1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. IPR-803

IPR-803 

Cat. No.: HY-111192
Handling Instructions

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.

For research use only. We do not sell to patients.

IPR-803 Chemical Structure

IPR-803 Chemical Structure

CAS No. : 892243-35-5

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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].

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].

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.
Molecular Weight

453.49

Formula

C₂₇H₂₃N₃O₄

CAS No.

892243-35-5

SMILES

O=C(O)C1=CC=CC(NC2=C(C3=C4ON=C3C(N5CCCCCC5)=C2)C(C6=C4C=CC=C6)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

IPR-803IPR803IPR 803Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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