1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. 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.

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 275 In-stock
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10 mM * 1 mL in DMSO USD 275 In-stock
Solid
5 mg USD 250 In-stock
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100 mg USD 2048 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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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]

Cellular Effect
Cell Line Type Value Description References
A549 IC50
> 10 μM
Compound: 2, IPR-803
Inhibition of cell invasion in human A549 cells after 16 hrs by matrigel assay
Inhibition of cell invasion in human A549 cells after 16 hrs by matrigel assay
[PMID: 22771232]
NCI-H1299 IC50
> 10 μM
Compound: 2, IPR-803
Inhibition of cell invasion in human H1299 cells after 16 hrs by matrigel assay
Inhibition of cell invasion in human H1299 cells after 16 hrs by matrigel assay
[PMID: 22771232]
NCI-H1299 IC50
50 μM
Compound: 2, IPR-803
Inhibition of cell migration in human H1299 cells after 16 hrs by Boyden chamber analysis
Inhibition of cell migration in human H1299 cells after 16 hrs by Boyden chamber analysis
[PMID: 22771232]
NCI-H460 IC50
> 10 μM
Compound: 2, IPR-803
Inhibition of cell invasion in human H460 cells after 16 hrs by matrigel assay
Inhibition of cell invasion in human H460 cells after 16 hrs by matrigel assay
[PMID: 22771232]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (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[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.
Appearance

Solid

Color

Brown to reddish brown

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.69 mg/mL (16.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2051 mL 11.0256 mL 22.0512 mL
5 mM 0.4410 mL 2.2051 mL 4.4102 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.77 mg/mL (1.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 5 mg/mL (11.03 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: ≥98.0%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2051 mL 11.0256 mL 22.0512 mL 55.1280 mL
5 mM 0.4410 mL 2.2051 mL 4.4102 mL 11.0256 mL
10 mM 0.2205 mL 1.1026 mL 2.2051 mL 5.5128 mL
15 mM 0.1470 mL 0.7350 mL 1.4701 mL 3.6752 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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IPR-803
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