| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
IC50: 27.8 nM (STAT3 luciferase activity)[1]
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| ln Vitro |
In MKN45, AGS, and MGC803 cells, HP590 (0–40 μM; 72 h) has anti-proliferative properties[1]. GC cells' phosphorylation of STAT3 Tyr705 and Ser727 is inhibited by HP590 (0–40 nM; 0–24 h); GC cells' production of STAT3 downstream genes (c-Myc and cyclin D1) is blocked; and MKN45 cells' IL-6-mediated STAT3 nuclear translocation is decreased[1]. Apoptosis in gastric cancer cells is induced by HP590 (5–20 nM; 48 h)[1].
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| ln Vivo |
HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) efficiently prevents GC growth by blocking STAT3 activation, and the GC xenograft model exhibits improved tolerance as a result[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MKN45, AGS, and MGC803 cells Tested Concentrations: 0-40 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited MKN45, AGS, and MGC803 cells with IC50s of 9.3, 13.5, and 8.7 nM, respectively. Apoptosis Analysis[1] Cell Types: MKN45 and AGS cells Tested Concentrations: 5, 10, and 20 nM Incubation Duration: 48 hrs (hours) Experimental Results: Induced apoptosis in MKN45 and AGS cells in a dose-dependent manner. Western Blot Analysis[1] Cell Types: Gastric Cancer Cells Tested Concentrations: 0-40 nM Incubation Duration: 0-24 h Experimental Results: 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. demonstrated the STAT3 p-Tyr705 stimulated by IL-6 in GC cell lines, but entirely suppressed by HP590 at 40 nM. RT-PCR[1] Cell Types: MKN45 and AGS cells Tested Concentrations: 10, 20, and 40 nM Incubation Duration: 48 hrs (hours) Experimental Results: Suppressed the expression of STAT3 downstream genes (c-Myc and |
| Animal Protocol |
Animal/Disease Models: BALB/c-nude mice injected with GC cells[1]
Doses: 25 and 50 mg/kg Route of Administration: Oral administration; 25 and 50 mg/kg; one time/day; 5 weeks Experimental Results: Inhibited MKN45 tumor growth in a concentration-dependent manner. Inhibited STAT3 phosphorylation at Tyr705 and Ser727 and decreased the expression of the downstream genes. Inhibited the expression of Ki67 (a proliferation marker). demonstrated no weight loss during HP590 treatment, and no apparent damage in the major organs of mice. |
| References |
[1]. He P, et al. Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr705/Ser727 Inhibitory Activity for Gastric Cancer Treatment. J Med Chem. 2022 Sep 14.
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| Molecular Formula |
C29H24F6N4O3
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|---|---|
| Molecular Weight |
590.52
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| Solubility (In Vitro) |
DMSO :~5 mg/mL (~8.47 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (0.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.5 mg/mL (0.85 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6934 mL | 8.4671 mL | 16.9342 mL | |
| 5 mM | 0.3387 mL | 1.6934 mL | 3.3868 mL | |
| 10 mM | 0.1693 mL | 0.8467 mL | 1.6934 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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