1. PI3K/Akt/mTOR Apoptosis
  2. PI3K Apoptosis
  3. HS-173

HS-173 is a novel PI3K inhibitor, that is used for cancer treatment.

For research use only. We do not sell to patients.

HS-173 Chemical Structure

HS-173 Chemical Structure

CAS No. : 1276110-06-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
1 mg USD 45 In-stock
5 mg USD 95 In-stock
10 mg USD 150 In-stock
25 mg USD 280 In-stock
50 mg USD 450 In-stock
100 mg   Get quote  
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

HS-173 is a novel PI3K inhibitor, that is used for cancer treatment.

IC50 & Target[4]

PI3Kα

0.8 nM (IC50)

In Vitro

HS-173 (0.1-10 μM) reduces the cell viability in a dose- and time-dependent manner. HS-173 shows a significant drug response by the inhibition of colony formation in pancreatic cancer cells dose-dependently. HS-173 inhibits TGF-β-induced cell migration and invasion in pancreatic cancer cells. HS-173 suppresses TGF-β-induced epithelial mesenchymal transition (EMT)[1]. HS-173 treatment reduces cell viability in two hepatic stellate cell lines in a dose and time dependent manner. HS-173 induces cell cycle arrest in the G2/M phase. HS-173 treatment increases the expression of cleaved caspase-3 and decreased that of Bcl-2 in the HSC-T6 cells. HS-173 inhibits the expression of profibrotic mediators and ECM degradation modulators in HSCs[2]. The combination of Sorafenib and HS-173 synergistically inhibits cell proliferation in pancreatic cancer cell lines. The combination of Sorafenib and HS-173 inhibits key enzymes in both RAF/MAPK and PI3K/AKT signaling pathways[3].

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

In Vivo

HS-173 (10 mg/kg, i.p.) significantly increases expression of TUNEL, cleaves caspase-3 along with decreased expression of PCNA in tumor tissues. HS-173 treatment decreases p-AKT and p-Smad2 in tumor tissues. HS-173 (10 and 30 mg/kg) significantly decreases the metastatic burdens on the lung and liver[1]. HS-173 (10 and 20?mg/kg) inhibits ECM accumulation and PI3K/Akt signaling in mice with CCl4-induced liver fibrosis animal model. HS-173 clearly suppresses the expression of p-Akt and p-P70S6K along with decreasing expression of collagen I and vimentin in the mice with CCl4-induced liver fibrosis[2].

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

Molecular Weight

422.46

Formula

C21H18N4O4S

CAS No.
Appearance

Solid

Color

White to gray

SMILES

O=C(C1=CN=C2C=CC(C3=CC(NS(=O)(C4=CC=CC=C4)=O)=CN=C3)=CN21)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (118.35 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 2.3671 mL 11.8354 mL 23.6709 mL
5 mM 0.4734 mL 2.3671 mL 4.7342 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.92 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (25.0 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: 2.5 mg/mL (5.92 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 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 (25.0 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:

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: 99.04%

References
Cell Assay
[1]

Cell viability is performed using an MTT assay. In brief, cells are seeded at a density of 5000-7000 cells/well in a 96-well plates following to 24 h incubation. On the following day the media are removed and the cells are treated with either vehicle as a negative control or various concentrations of HS-173 (0.5-10 μM) following an incubation for 24, 48, or 72 h. After incubation of respective time 10% of an MTT solution (2 mg/mL) is added to each well and the cells are incubated for another 4 h at 37°C. The formazan crystals that formed are dissolved in DMSO (100 or 300 μL/well) with constant shaking for 5 min. The absorbance of the plate is then read with a microplate reader at 540 nm. Three replicate wells are evaluated for each analysis.

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

Animal Administration
[1]

Male BALB/c mice (4 week old, weighing 18-20 g) are fed with standard rat chow and tap water ad libitum, and are maintained with a 12 h dark/light cycle at 21°C. After one week of adaptation period, Panc-1 cells (5×106 cells/mice) are inoculated in the right flank of the mouse. After reaching an average tumor volume of 50 mm3, mice are randomly divided into two groups with five mice in each group; the control group is treated with vehicle and the experimental group is treated with HS-173 (10 mg/kg) intraperitoneally thrice a week for 26 days. The body weight and tumor size are measured thrice a week. At the end of the experiment, mice are sacrificed and primary tumor is harvested. Tumors are weighed, photographed, and divided into two parts for Western blot and IHC analysis. For IHC analysis, tissues are immediately fixed in 4% PFA for overnight and for Western blotting analysis, tissues are snap-frozen in liquid nitrogen.

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3671 mL 11.8354 mL 23.6709 mL 59.1772 mL
5 mM 0.4734 mL 2.3671 mL 4.7342 mL 11.8354 mL
10 mM 0.2367 mL 1.1835 mL 2.3671 mL 5.9177 mL
15 mM 0.1578 mL 0.7890 mL 1.5781 mL 3.9451 mL
20 mM 0.1184 mL 0.5918 mL 1.1835 mL 2.9589 mL
25 mM 0.0947 mL 0.4734 mL 0.9468 mL 2.3671 mL
30 mM 0.0789 mL 0.3945 mL 0.7890 mL 1.9726 mL
40 mM 0.0592 mL 0.2959 mL 0.5918 mL 1.4794 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 1.1835 mL
60 mM 0.0395 mL 0.1973 mL 0.3945 mL 0.9863 mL
80 mM 0.0296 mL 0.1479 mL 0.2959 mL 0.7397 mL
100 mM 0.0237 mL 0.1184 mL 0.2367 mL 0.5918 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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HS-173
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