HS-173

novel PI3K inhibitor CAS# 1276110-06-5

HS-173

Catalog No. BCC5363----Order now to get a substantial discount!

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Chemical structure

HS-173

3D structure

Chemical Properties of HS-173

Cas No. 1276110-06-5 SDF Download SDF
PubChem ID 52936849 Appearance Powder
Formula C21H18N4O4S M.Wt 422.46
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 50 mg/mL (118.35 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name ethyl 6-[5-(benzenesulfonamido)pyridin-3-yl]imidazo[1,2-a]pyridine-3-carboxylate
SMILES CCOC(=O)C1=CN=C2N1C=C(C=C2)C3=CC(=CN=C3)NS(=O)(=O)C4=CC=CC=C4
Standard InChIKey SEKOTFCHZNXZMM-UHFFFAOYSA-N
Standard InChI InChI=1S/C21H18N4O4S/c1-2-29-21(26)19-13-23-20-9-8-15(14-25(19)20)16-10-17(12-22-11-16)24-30(27,28)18-6-4-3-5-7-18/h3-14,24H,2H2,1H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of HS-173

DescriptionHS-173 is a potent inhibitor of PI3Kα with IC50 value of 0.8 nM.
TargetsPI3Kα    
IC500.8 nM     

Protocol

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.

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.

References:
[1]. Rumman M, et al. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Oct 25. [2]. Son MK, et al. HS-173, a novel PI3K inhibitor, attenuates the activation of hepatic stellate cells in liver fibrosis. Sci Rep. 2013 Dec 11;3:3470. [3]. Yun SM, et al. Synergistic anticancer activity of HS-173, a novel PI3K inhibitor in combination with Sorafenib against pancreatic cancer cells. Cancer Lett. 2013 May 1;331(2):250-61. [4]. Kim O, et al. Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. J Med Chem. 2011 Apr 14;54(7):2455-66.

HS-173 Dilution Calculator

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HS-173 Molarity Calculator

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Preparing Stock Solutions of HS-173

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3671 mL 11.8354 mL 23.6709 mL 47.3418 mL 59.1772 mL
5 mM 0.4734 mL 2.3671 mL 4.7342 mL 9.4684 mL 11.8354 mL
10 mM 0.2367 mL 1.1835 mL 2.3671 mL 4.7342 mL 5.9177 mL
50 mM 0.0473 mL 0.2367 mL 0.4734 mL 0.9468 mL 1.1835 mL
100 mM 0.0237 mL 0.1184 mL 0.2367 mL 0.4734 mL 0.5918 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on HS-173

Phosphatidylinositol 3-kinase (PI3K) was first identified over 20 years ago as a lipid kinase associated with viral oncoproteins. PI3K signaling pathway regulates various cellular processes such as growth, cell cycle progression, apoptosis, migration, metabolism, and cytoskeleton rearrangement. HS-173 is a novel PI3K inhibitor.

In vitro: HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G2/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1a and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro [1].

In vivo: HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. These results suggest that HS-173 has potent anti-angiogenic activity in vivo [1].

Clinical trials: Currenlty no clinical data are available.

Reference:
[1] Lee H, Jung KH, Jeong Y, Hong S, Hong SS.   HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis. Cancer Lett. 2013 Jan 1;328(1):152-9.

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References on HS-173

HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer.[Pubmed:27793006]

Oncotarget. 2016 Nov 22;7(47):78029-78047.

Pancreatic cancer is one of the most aggressive solid malignancies prone to metastasis. Epithelial-mesenchymal transition (EMT) contributes to cancer invasiveness and drug resistance. In this study, we investigated whether HS-173, a novel PI3K inhibitor blocked the process of EMT in pancreatic cancer. HS-173 inhibited the growth of pancreatic cancer cells in a dose- and time-dependent manner. Moreover, it significantly suppressed the TGF-beta-induced migration and invasion, as well as reversed TGF-beta-induced mesenchymal cell morphology. Also, HS-173 reduced EMT by increasing epithelial markers and decreasing the mesenchymal markers by blocking the PI3K/AKT/mTOR and Smad2/3 signaling pathways in pancreatic cancer cells. In addition, HS-173 clearly suppressed tumor growth without drug toxicity in both xenograft and orthotopic mouse models. Furthermore, to explore the anti-metastatic effect of HS-173, we established pancreatic cancer metastatic mouse models and found that it significantly inhibited metastatic dissemination of the primary tumor to liver and lung. Taken together, our findings demonstrate that HS-173 can efficiently suppress EMT and metastasis by inhibiting PI3K/AKT/mTOR and Smad2/3 signaling pathways, suggesting it can be a potential candidate for the treatment of advanced stage pancreatic cancer.

HS-173, a novel PI3K inhibitor, attenuates the activation of hepatic stellate cells in liver fibrosis.[Pubmed:24326778]

Sci Rep. 2013 Dec 11;3:3470.

Hepatic stellate cells (HSCs) are the primary source of matrix components in liver disease such as fibrosis. Phosphatidylinositol 3-kinase (PI3K) signaling in HSCs has been shown to induce fibrogenesis. In this study, we evaluated the anti-fibrotic activity of a novel imidazopyridine analogue (HS-173) in human HSCs as well as mouse liver fibrosis. HS-173 strongly suppressed the growth and proliferation of HSCs and induced the arrest at the G2/M phase and apoptosis in HSCs. Furthermore, it reduced the expression of extracellular matrix components such as collagen type I, which was confirmed by an in vivo study. We also observed that HS-173 blocked the PI3K/Akt signaling pathway in vitro and in vivo. Taken together, HS-173 suppressed fibrotic responses such as cell proliferation and collagen synthesis by blocking PI3K/Akt signaling. Therefore, we suggest that this compound may be an effective therapeutic agent for ameliorating liver fibrosis through the inhibition of PI3K signaling.

HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis.[Pubmed:22929971]

Cancer Lett. 2013 Jan 1;328(1):152-9.

We synthesized a novel imidazopyridine analogue, a PI3Kalpha inhibitor HS-173 and investigated anti-cancer capacity in human cancer cells. HS-173 inhibited the PI3K signaling pathway, and showed anti-proliferative effects on cancer cells. Also, HS-173 induced cell cycle arrest at the G(2)/M phase and apoptosis. In addition, HS-173 decreased the expression HIF-1alpha and VEGF which play an important role in angiogenesis. This effect was confirmed by the suppression of tube formation and migration assay in vitro. Furthermore, HS-173 diminished blood vessel formation in the Matrigel plug assay in mice. Therefore, HS-173 is considered as a novel drug candidate to treat cancer patients.

Synergistic anticancer activity of HS-173, a novel PI3K inhibitor in combination with Sorafenib against pancreatic cancer cells.[Pubmed:23340175]

Cancer Lett. 2013 May 1;331(2):250-61.

The RAF/MEK/ERK and PI3K/AKT pathways are highly implicated in the development of pancreatic cancer. The principal objective of this study was to assess the synergic effect between Sorafenib (a RAF inhibitor) and HS-173 (a novel PI3K inhibitor) to gain insight into novel therapeutic strategies for treating pancreatic cancer. We first investigated the cytotoxic effect of co-treatment with Sorafenib and HS-173 using the Calcusyn program. Combined treatment of the two drugs synergistically inhibited the viability of Panc-1 cells (combination index<1). Concomitantly, the co-treatment induced G2/M arrest and increased apoptosis with the loss of mitochondrial membrane potential. Apoptosis resulting from the co-treatment was accompanied by increased levels of cleaved caspase-3 and PARP as well as greater numbers of TUNEL-positive apoptotic cells compared to treatment with either drug alone. Furthermore, combined treatment with these drugs decreased the expression of HIF-1alpha and VEGF which play an important role in angiogenesis. This anti-angiogenic effect was confirmed by the suppressed tube formation of VEGF-induced human umbilical vein endothelial cells and inhibition of blood vessel formation in a Matrigel plug assay in mice. Taken together, our study demonstrates that combined treatment with Sorafenib and HS-173 has a synergistic anti-cancer effect on pancreatic cancer cells, indicating that simultaneously targeting the RAF/MEK and PI3K/AKT pathways can induce a synergistic inhibitory effect on pancreatic cancers in which both pathways are activated. Based on the observations from our study, we suggest that the combined administration of these two drugs may be considered to be a new therapeutic regimen for treating pancreatic cancer.

Description

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

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