IPR-803
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.0%
- No. CAS: 892243-35-5
- Fòrmula: C27H23N3O4
- Peso molecular:453.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) IPR-803
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Actividad biológica
Ki: 0.2 μM (PPI)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10 μM
Compound: 2, IPR-803
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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
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[PMID: 22771232] |
| NCI-H1299 | IC50 |
>10 μM
Compound: 2, IPR-803
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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
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[PMID: 22771232] |
| NCI-H1299 | IC50 |
50 μM
Compound: 2, IPR-803
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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
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[PMID: 22771232] |
| NCI-H460 | IC50 |
>10 μM
Compound: 2, IPR-803
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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
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[PMID: 22771232] |
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.
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Cell Line:MDA-MB-231 cells
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Concentration:0 μM, 50 μM, 150 μM, 200 μM
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Incubation Time:3 days
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Result:Displays 90 percent blockage of invasion that is observed at 50 μM.
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.
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Animal Model:NSG mice with MDA-MB-231 cells xenograft[1]
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Dosage:200 mg/kg
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Administration:Oral gavage; three times a week; for 5 weeks
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Result:Impaired metastasis to the lungs.
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Animal Model:NOD/SCID mice[1]
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Dosage:200 mg/kg (Pharmacokinetic Study)
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Administration:Oral administration
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Result:t1/2=5 hours.
Chemical Information
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No. CAS 892243-35-5
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Appearance Solid
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Peso molecular 453.49
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Fòrmula C27H23N3O4
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Color Brown to reddish brown
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SMILES
O=C(O)C1=CC=CC(NC2=C(C3=C4ON=C3C(N5CCCCCC5)=C2)C(C6=C4C=CC=C6)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (11.03 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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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