HS-173

• CAS: 1276110-06-5
• Catalog Number: ACM1276110065
• Category: Inhibitors
• Molecular Weight: 422.46
• Molecular Formula: C21H18N4O4S
• 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.
• Synonyms: HS173; HS 173; HS-173
• IUPAC Name: ethyl 6-(5-(phenylsulfonamido)pyridin-3-yl)imidazo[1,2-a]pyridine-3-carboxylate
• Canonical SMILES: O=C(C1=CN=C2C=CC(C3=CC(NS(=O)(C4=CC=CC=C4)=O)=CN=C3)=CN21)OCC
• 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
• InChI Key: SEKOTFCHZNXZMM-UHFFFAOYSA-N
• Solubility: soluble in DMSO, not soluble in water
• Appearance: White to off-white solid powder
• Shelf Life: >2 years if stored properly
• Storage: 0-4 °C for short term (weeks to 1 month) or -20 °C for long terms (months to years).
• Biological Target: HS-173 is a PI3Kα inhibitor with IC50 of 0.8 nM.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 59.70; H, 4.29; N, 13.26; O, 15.15; S, 7.59
• Exact Mass: 422.10488
• HS Tariff Code: 2934.99.9001
• 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/
• Shipping: 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.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).