GLPBio

IPR-803

Catalog No.: GC39713Purity:>98.00%
COASDSData Sheet
IPR-803 is a small molecule inhibitor of urokinase receptor (uPAR). IPR-803 competitively blocks the protein-protein interaction between uPAR and urokinase-type plasminogen activator (uPA).

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IPR-803
Cas No.: 892243-35-5
10mM (in 1mL DMSO)In Stock
$248.00
1
1mgIn Stock
$75.00
1
5mgIn Stock
$225.00
1
10mgIn Stock
$360.00
1
25mgIn Stock
$720.00
1
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Description

IPR-803 is a small molecule inhibitor of urokinase receptor (uPAR). IPR-803 competitively blocks the protein-protein interaction between uPAR and urokinase-type plasminogen activator (uPA). IPR-803 downregulates uPA expression. IPR-803 inhibits MMP-mediated extracellular matrix degradation and p-ERK/MAPK signaling. IPR-803 reduces angiogenesis and metastasis. IPR-803 is used for studying metastasis in breast cancer and pancreatic cancer[1-4].

In vitro, MDA-MB-231 cells were treated with 0-100μM IPR-803 for 0.5-16 hours. IPR-803 inhibited cell invasion and proliferation in a concentration-dependent manner[5]. RKO cells were treated with 30μM IPR-803 for 48-6 hours. IPR-803 inhibited phosphorylation of FAK and SLC6A8 proteins[6].

In vivo, female NSG mice with mammary fat pad inoculation of TMD-MDA-MB-231 cells received daily oral gavage of 200mg/kg IPR-803 for 33 days. IPR-803 inhibited breast cancer cell metastasis to the lungs[7]. Tumor-bearing nude mice with KYSE-450 cells received oral gavage of 50mg/kg IPR-803 every 3 days for 24 days. IPR-803 inhibited tumor growth[8].

References:
[1] Liu D, Zhou D, Wang B, et al. A new class of orthosteric uPAR·uPA small-molecule antagonists are allosteric inhibitors of the uPAR·vitronectin interaction. ACS Chem Biol. 2015 Jun 19;10(6):1521-34.
[2] Montuori N, Pesapane A, Rossi FW, et al. Urokinase type plasminogen activator receptor (uPAR) as a new therapeutic target in cancer. Transl Med UniSa. 2016 Nov 1;15:15-21.
[3] Li Santi A, Napolitano F, Montuori N, et al. The Urokinase Receptor: A Multifunctional Receptor in Cancer Cell Biology. Therapeutic Implications. Int J Mol Sci. 2021 Apr 16;22(8):4111.
[4] Zhou J, Ma S, Feng D, et al. C5aR1+ microglia exacerbate neuroinflammation and cerebral edema in acute brain injury. Neuron. 2026 Feb 4;114(3):444-462.e9.
[5] Khanna M, Wang F, Jo I, et al. Targeting Multiple Conformations Leads to Small Molecule Inhibitors of the uPAR·uPA Protein-Protein Interaction that Block Cancer Cell Invasion. ACS Chem Biol. 2011 Nov 18;6(11):1106-16.
[6] Yu J, Xiu M, Yu S, et al. The Role of CAF-derived Vitronectin in Promoting Colorectal Cancer Progression and Immunosuppression. Adv Sci (Weinh). 2025 Sep;12(33):e05769.
[7] Mani T, Wang F, Knabe WE, 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.
[8] Fang L, Che Y, Zhang C, et al. PLAU directs conversion of fibroblasts to inflammatory cancer-associated fibroblasts, promoting esophageal squamous cell carcinoma progression via uPAR/Akt/NF-kB/IL8 pathway. Cell Death Discovery. 2021 Feb 11;7(1):32.

Protocol

Cell experiment [1]:

Cell lines

 MDA-MB-231 cells (human breast cancer cell line)

Preparation Method

 MDA-MB-231 cells were treated with IPR-803, then invasion through fibronectin-coated transwell, migration by Boyden chamber and wound healing, adhesion to fibronectin/vitronectin, surface uPA/uPAR staining, and proliferation/toxicity by MTT were measured.

Reaction Conditions

 0-100μM; 0.5-16h

Applications

 IPR-803 reduced MDA-MB-231 invasion through membrane, showed weak/no effect on migration and no effect on adhesion, reduced surface uPA binding to uPAR, and caused concentration-dependent reduction in cell proliferation.
Animal experiment [2]:

Animal models

 Female NSG mice

Preparation Method

TMD-MDA-MB-231 cells were inoculated into the mammary fat pads of female NSG mice. Dosing was initiated at day 15 post implantation. Animals were randomized and treated with vehicle or with IPR-803 by daily oral gavage at a dose of 200mg/kg for 33 days. Tumor volumes were determined by caliper measurements on a twice weekly basis. At the end of the study, animals were sacrificed and lungs were removed for H&E staining and metastasis scoring.

Dosage form

200mg/kg; p.o.; daily for 33 days

Applications

IPR-803 impaired breast cancer metastasis to the lungs. IPR-803 had little effect on primary tumor growth and no significant effect on body weight.
References:
[1] Khanna M, Wang F, Jo I, et al. Targeting Multiple Conformations Leads to Small Molecule Inhibitors of the uPAR·uPA Protein-Protein Interaction that Block Cancer Cell Invasion. ACS Chem Biol. 2011 Nov 18;6(11):1108-18.
[2] Mani T, Wang F, Knabe WE, 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

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
Molecular Formula
C27H23N3O4
Molecular Weight
453.49
Solubility
Soluble in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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