1. PI3K/Akt/mTOR
  2. PI3K

HS-173 

Cat. No.: HY-15868 Purity: 99.32%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 106 In-stock
5 mg USD 96 In-stock
10 mg USD 168 In-stock
25 mg USD 348 In-stock
50 mg USD 540 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 0.8 nM (PI3Kα)[1]

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].

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].

References
Preparing Stock Solutions
Concentration Volume 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
10 mM 0.2367 mL 1.1835 mL 2.3671 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

HS-173 is dissolved in DMSO at 20 mM stock concentration.

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]

HS-173 is dissolved in DPBS: PEG400:DMSO (4:5:1).

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
Molecular Weight

422.46

Formula

C₂₁H₁₈N₄O₄S

CAS No.

1276110-06-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 26 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.32%

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Product Name:
HS-173
Cat. No.:
HY-15868
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