HS-173


Catalog No. size PriceQuantity
M7111-2 2mg solid $90
M7111-10 10mg solid $360

Description

Cas:1276110-06-5

Product Information

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 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

 

Synonym: 

 

HS173

HS 173

HS-173

 

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

 

 

Technical Data:

 

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

 

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). 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.

 

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. 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.

 

 

References

 

  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.

 

  1. 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.

 

  1. 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.

 

  1. 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.

 

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

 

Products are for research use only. Not for human use.

 

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