2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. HP590

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.

HP590 Chemical Structure

HP590 Chemical Structure

CAS No. : 2971855-37-3

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Description

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[1].

IC50 & Target

IC50: 27.8 nM (STAT3 luciferase activity)[1]
In Vitro

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.

HP590 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MKN45, AGS, and MGC803 cells
Concentration: 0-40 μM
Incubation Time: 72 hours
Result: Inhibited MKN45, AGS, and MGC803 cells with IC50s of 9.3, 13.5, and 8.7 nM, respectively.

Apoptosis Analysis[1]

Cell Line: MKN45 and AGS cells
Concentration: 5, 10, and 20 nM
Incubation Time: 48 hours
Result: Induced apoptosis in MKN45 and AGS cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Gastric Cancer Cells
Concentration: 0-40 nM
Incubation Time: 0-24 h
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.

RT-PCR[1]

Cell Line: MKN45 and AGS cells
Concentration: 10, 20, and 40 nM
Incubation Time: 48 hours
Result: Suppressed the expression of STAT3 downstream genes (c-Myc and cyclin D1) at the mRNA level.
In Vivo

HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model[1].

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

Animal Model: BALB/c-nude mice injected with GC cells[1]
Dosage: 25 and 50 mg/kg
Administration: Oral administration; 25 and 50 mg/kg; once daily; 5 weeks
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.
Molecular Weight

590.52

Formula

C29H24F6N4O3
CAS No.
Appearance

Solid

Color

White to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
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:
%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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
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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HP590 Related Classifications

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.

Keywords:

HP5902971855-37-3HP 590HP-590STATApoptosisanti-proliferative activitygastric cancer cellsapoptosisMKN45AGSMGC803Inhibitorinhibitorinhibit

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