HS-173
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MedKoo CAT#: 406355

CAS#: 1276110-06-5

Description: HS-173 is a potent PI3Kα inhibitor with potential anticancer activity. 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-1α 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.


Chemical Structure

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HS-173
CAS# 1276110-06-5

Theoretical Analysis

MedKoo Cat#: 406355
Name: HS-173
CAS#: 1276110-06-5
Chemical Formula: C21H18N4O4S
Exact Mass: 422.10488
Molecular Weight: 422.46
Elemental Analysis: C, 59.70; H, 4.29; N, 13.26; O, 15.15; S, 7.59

Price and Availability

Size Price Availability Quantity
10.0mg USD 120.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 750.0 Ready to ship
200.0mg USD 1250.0 Ready to ship
500.0mg USD 2250.0 Ready to ship
1.0g USD 3250.0 Ready to ship
2.0g USD 5650.0 2 weeks
5.0g USD 7950.0 2 weeks
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Synonym: HS173; HS 173; HS-173.

IUPAC/Chemical Name: ethyl 6-(5-(phenylsulfonamido)pyridin-3-yl)imidazo[1,2-a]pyridine-3-carboxylate

InChi Key: SEKOTFCHZNXZMM-UHFFFAOYSA-N

InChi Code: 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

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

Appearance: white to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs

Storage Condition: 0 – 4 C for short term (weeks to 1 month) or -20 C for long terms (months to years).

Solubility: soluble in DMSO, not soluble in water.

Shelf Life: >2 years if stored properly.

Drug Formulation: this drug may be formulated in DMSO.

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: HS-173 is a PI3Kα inhibitor with IC50 of 0.8 nM.
In vitro activity: In order to evaluate the effect of HS-173 on the cell growth of pancreatic cancer, three cell lines (Panc-1, Miapaca-2 and Aspc-1) were used. When pancreatic cancer cells were treated with various concentrations (0.1-10 μM) of HS-173, it reduced the cell viability in a dose- and time-dependent manner (Figure 1A). In particular, 1 μM of HS-173 inhibited the cell growth by 40-50% in Miapaca-2 and Aspc-1 cells at 48 h. To further determine the sensitivity of HS-173, clonogenic assay was performed in Miapaca-2 cells for 14 days. In agreement with the MTT assay, HS-173 showed a significant drug response by the inhibition of colony formation in pancreatic cancer cells dose-dependently. Additionally, it was observed that colony formation by HS-173 was less than 50% in Miapaca-2 cells at dose of 1 μM (Figure 1B). Reference: Oncotarget. 2016 Nov 22;7(47):78029-78047. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5363641/
In vivo activity: To determine whether HS-173 is involved in tumorigenesis in vivo, xenograft and orthotopic pancreatic tumor models were used in the Balb/c nude mice. HS-173 dramtically reduced tumor volume and weight, compared with the control group in two mouse models (Figure 6A and 6B). Also, HS-173 significantly increased expression of TUNEL, cleaved caspase-3 along with decreased expression of PCNA in tumor tissues (Figure 6C). To further confirm whether or not HS-173 inhibits tumor growth through the regulation of EMT, the expression levels of Ecadherin, Vimentin, ZEB1 along with p-AKT and p-Smad2 were identified. Ecadherin was increased, whereas Vimentin and ZEB1 were downregulated in the HS-173 treated group (Figure 6D and 6E). Furthermore, HS-173 treatment decreased p-AKT and p-Smad2 in tumor tissues. These results demonstrate that HS-173 has potent anti-tumor efficacy by inhibiting EMT via regulation of PI3K/AKT and TGF/Smads pathways. Reference: Oncotarget. 2016 Nov 22;7(47):78029-78047. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5363641/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 53.0 125.46
DMF 25.0 59.18
DMF:PBS (pH 7.2) (1:1) 0.5 1.18
Ethanol 1.0 2.37

Preparing Stock Solutions

The following data is based on the product molecular weight 422.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Foki E, Stanisz I, Kadletz L, Kotowski U, Seemann R, Schmid R, Heiduschka G. HS-173, a selective PI3K inhibitor, induces cell death in head and neck squamous cell carcinoma cell lines. Wien Klin Wochenschr. 2021 Jan;133(1-2):26-31. doi: 10.1007/s00508-020-01729-3. Epub 2020 Sep 2. PMID: 32876741. 2. Rumman M, Jung KH, Fang Z, Yan HH, Son MK, Kim SJ, Kim J, Park JH, Lim JH, Hong S, Hong SS. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Nov 22;7(47):78029-78047. doi: 10.18632/oncotarget.12871. PMID: 27793006; PMCID: PMC5363641.
In vitro protocol: 1. Foki E, Stanisz I, Kadletz L, Kotowski U, Seemann R, Schmid R, Heiduschka G. HS-173, a selective PI3K inhibitor, induces cell death in head and neck squamous cell carcinoma cell lines. Wien Klin Wochenschr. 2021 Jan;133(1-2):26-31. doi: 10.1007/s00508-020-01729-3. Epub 2020 Sep 2. PMID: 32876741. 2. Rumman M, Jung KH, Fang Z, Yan HH, Son MK, Kim SJ, Kim J, Park JH, Lim JH, Hong S, Hong SS. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Nov 22;7(47):78029-78047. doi: 10.18632/oncotarget.12871. PMID: 27793006; PMCID: PMC5363641.
In vivo protocol: 1. Rumman M, Jung KH, Fang Z, Yan HH, Son MK, Kim SJ, Kim J, Park JH, Lim JH, Hong S, Hong SS. HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. Oncotarget. 2016 Nov 22;7(47):78029-78047. doi: 10.18632/oncotarget.12871. PMID: 27793006; PMCID: PMC5363641.

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1: Son MK, Ryu YL, Jung KH, Lee H, Lee HS, Yan HH, Park HJ, Ryu JK, Suh JK, Hong S, Hong SS. HS-173, a novel PI3K inhibitor, attenuates the activation of hepatic stellate cells in liver fibrosis. Sci Rep. 2013 Dec 11;3:3470. doi: 10.1038/srep03470. PubMed PMID: 24326778; PubMed Central PMCID: PMC3858860.

2: Lee H, Kim SJ, Jung KH, Son MK, Yan HH, Hong S, Hong SS. A novel imidazopyridine PI3K inhibitor with anticancer activity in non-small cell lung cancer cells. Oncol Rep. 2013 Aug;30(2):863-9. doi: 10.3892/or.2013.2499. Epub 2013 May 27. PubMed PMID: 23708425.

3: Jung KH, Ryu YL, Lee HS, Lee H, Son MK, Yan HH, Hong SW, Ryu JK, Hong S, Suh JK, Hong SS. A novel PI3K inhibitor alleviates fibrotic responses in fibroblasts derived from Peyronie's plaques. Int J Oncol. 2013 Jun;42(6):2001-8. doi: 10.3892/ijo.2013.1905. Epub 2013 Apr 16. PubMed PMID: 23588860.

4: Yun SM, Jung KH, Lee H, Son MK, Seo JH, Yan HH, Park BH, Hong S, Hong SS. 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. doi: 10.1016/j.canlet.2013.01.007. Epub 2013 Jan 20. PubMed PMID: 23340175.

5: 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. doi: 10.1016/j.canlet.2012.08.020. Epub 2012 Aug 26. PubMed PMID: 22929971.

HS-173

10.0mg / USD 120.0


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