Home PI3K/Akt/mTOR PI3K inhibitor HS-173 For research use only.

HS-173

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

HS-173 Chemical Structure

HS-173 Chemical Structure

CAS No. 1276110-06-5

Purity & Quality Control

HS-173 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D cells Cytotoxicity assay 48 h Cytotoxicity against human T47D cells after 48 hrs by MTT assay, IC50=0.6 μM 21388141
SK-BR-3 cells Cytotoxicity assay 48 h Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay, IC50=1.5 μM 21388141
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=7.8 μM 21388141
Click to View More Cell Line Experimental Data

Biological Activity

Description HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
Features PI3Kα-selective inhibitor.
Targets
PI3Kα [1]
(cell-free assay)
0.8 nM
In vitro
In vitro

HS-173 shows potent antiproliferative effects in T47D, SK-BR3, and MCF7 cells with IC50 of 0.6, 1.5, and 7.8 μM, respectively. [1] HS-173 causes complete suppression of the PI3K pathway in cancer cell lines (Hep3B and SkBr3). Moreover, HS-173 induces cell apoptosis by affecting cell-cycle distribution and activating caspases, and block VEGF-induced angiogenesis in vitro. [2]
Kinase Assay PI3-Kinase assay
The PI3K assay is performed using the Kinase-Glo Max luminescent kinase assay kit which quantifies the amount of ADP produced by the PI3K reaction. In brief, an active PI3K (100 ng) is preincubated with compound for 5 min in kinase reaction buffer (25 mM MOPS [pH 7.0], 5 mM MgCl2, and 1 mM EGTA) and 10 μg l-α-phosphatidylinositol (PI). Before addition of PI, it is sonicated with sonication buffer (25 mM MOPS [pH 7.0], 1 mM EGTA) in water for 20 min for allowing miscelle formation. Then reaction is started by the addition of 10 μM ATP and ran for 180 min. To terminate kinase reaction, same volume of Kinase-Glo Max buffer is added. After 10 min, the plates are then read on a GloMax plate reader for luminescence detection.
Cell Research Cell lines T47D, SK-BR3, MCF7 cells
Concentrations ~50 μM
Incubation Time 48 hours
Method

Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated with either DMSO as a control or various concentrations of inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. The plate is then read on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose−response curves. To assess the effect of compounds on cell proliferation, T47D cells are cultured with compound (0.1−100 μM) for 48 h before MTT analysis.
In Vivo
In vivo

HS-173 diminishes blood vessel formation in mice. [2] HS-173 markedly attenuates the development of liver fibrosis by blocking PI3K/Akt signaling in vivo. [4]
Animal Research Animal Models Male BALB/c mice with CCl4-induced liver fibrosis
Dosages ~20 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 422.46 Formula

C21H18N4O4S
CAS No. 1276110-06-5 SDF Download HS-173 SDF
Smiles CCOC(=O)C1=CN=C2N1C=C(C=C2)C3=CC(=CN=C3)NS(=O)(=O)C4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (198.83 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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