HP590
Based on 1 Customer Validation
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis.
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 2971855-37-3
- Formula: C29H24F6N4O3
- Molecular Weight:590.52
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 27.8 nM (STAT3 luciferase activity)[1]
HP590 (0-40 μM; 72 h) shows anti-proliferative activities to MKN45, AGS, and MGC803 cells[1].
HP590 (0-40 nM; 0-24 h) inhibits STAT3 Tyr705 and Ser727 phosphorylation in GC cells, blocks the expression of STAT3 downstream genes (c-Myc and cyclin D1) in GC cells, reduces IL-6-mediated STAT3 nuclear translocation in MKN45 cells[1].
HP590 (5-20 nM; 48 h) induces gastric cancer cell apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN45, AGS, and MGC803 cells
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Concentration:0-40 μM
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Incubation Time:72 hours
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Result:Inhibited MKN45, AGS, and MGC803 cells with IC50s of 9.3, 13.5, and 8.7 nM, respectively.
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Cell Line:MKN45 and AGS cells
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Concentration:5, 10, and 20 nM
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Incubation Time:48 hours
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Result:Induced apoptosis in MKN45 and AGS cells in a dose-dependent manner.
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Cell Line:Gastric Cancer Cells
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Concentration:0-40 nM
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Incubation Time:0-24 h
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Result:Inhibited STAT3 p-Tyr705 and p-Ser727 in GC cells completely at 40 nM.
Blocked the expression of STAT3 downstream genes, including c-Myc and cyclin D1, in a concentration-dependent and time-dependent manner.
Showed the STAT3 p-Tyr705 stimulated by IL-6 in GC cell lines, but entirely suppressed by HP590 at 40 nM.
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Cell Line:MKN45 and AGS cells
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Concentration:10, 20, and 40 nM
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Incubation Time:48 hours
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Result:Suppressed the expression of STAT3 downstream genes (c-Myc and cyclin D1) at the mRNA level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-nude mice injected with GC cells[1]
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Dosage:25 and 50 mg/kg
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Administration:Oral administration; 25 and 50 mg/kg; once daily; 5 weeks
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Result:Inhibited MKN45 tumor growth in a concentration-dependent manner.
Inhibited STAT3 phosphorylation at Tyr705 and Ser727 and reduced the expression of the downstream genes.
Inhibited the expression of Ki67 (a proliferation marker).
Showed no weight loss during HP590 treatment, and no apparent damage in the major organs of mice.
Chemical Information
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CAS No. 2971855-37-3
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Appearance Solid
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Molecular Weight 590.52
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Formula C29H24F6N4O3
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Color White to light yellow
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SMILES
O=C(N1CCN(CC1)CC2=CC=C(C=C2)OCC(F)(F)F)C3=CC=C(C=C3)C4=NC(C5=CC=C(C=C5)C(F)(F)F)=NO4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 5 mg/mL (8.47 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.85 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.5 mg/mL (0.85 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 (sealed storage, away from moisture and light). 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 | 1.6934 mL | 8.4671 mL | 16.9342 mL | 42.3356 mL |
| 5 mM | 0.3387 mL | 1.6934 mL | 3.3868 mL | 8.4671 mL |
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