1276110-06-5

Basic information

• Product Name: HS-173
• Synonyms: HS-173;6-[5-[(Phenylsulfonyl)amino]-3-pyridinyl]imidazo[1,2-a]pyridine-3-carboxylic acid ethyl ester;ethyl 6-(5-(phenylsulfonamido)pyridin-3-yl)imidazo[1,2-a]pyridine-3-carboxylate;6-[5-[(Phenylsulfonyl)amino]-3-pyridinyl]imidazo[1,2-a]pyridine-3-carboxylic acid ethyl ester HS-173;HS-173, 98%, a novel PI3K inhibitor
• CAS NO: 1276110-06-5
• Molecular Formula: C₂₁H₁₈N₄O₄S
• Molecular Weight: 422.45702
• Product Categories: Inhibitors
• Mol File: 1276110-06-5.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• Density: 1.38±0.1 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• Solubility: Chloroform (Slightly), DMSO (Slightly)
• PKA: 6.84±0.40(Predicted)
• CAS DataBase Reference: HS-173(CAS DataBase Reference)
• NIST Chemistry Reference: HS-173(1276110-06-5)
• EPA Substance Registry System: HS-173(1276110-06-5)

Safety Data

• Hazardous Substances Data: 1276110-06-5(Hazardous Substances Data)

Usage

Description

HS-173 is an imidazopyridine analog that acts as a PI3Kα inhibitor with an IC50 value of 0.8 nM. It demonstrates antiproliferative activity in T47D, SK-BR-3, and MCF-7 cells with IC50 values of 0.6, 1.5, and 7.8 μM, respectively. HS-173 is reported to induce apoptosis by arresting the cell cycle at the G2/M phase and by activating caspases. It has also been shown to block VEGF-induced angiogenesis both in vitro and in vivo.

Uses

HS-173 is a potent PI3Kα inhibitor with anticancer activity.

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].

references

[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.

Upstream product

• 98-09-9 benzenesulfonyl chloride 
• 1084-12-4 N-(5-bromopyridin-3-yl)benzenesulfonamide 
• 372198-69-1 ethyl 6-bromoimidazol[1,2-a]pyridine-3-carboxylate 
• 1083326-28-6 N-(5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)-benzenesulfonamide 
• 1072-97-5 5-bromo-2-pyridylamine 
• 13535-01-8 3-amino-5-bromopyridine 

Relevant articles and documents

Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis

Phosphatidylinositol 3-kinase α (PI3Kα) is an important regulator of intracellular signaling pathways, controlling remarkably diverse arrays of physiological processes. Because the PI3K pathway is frequently up-regulated in human cancers, the inhibition of PI3Kα can be a promising approach to cancer therapy. In this study, we have designed and synthesized a new series of imidazo[1,2-a]pyridine derivatives as PI3Kα inhibitors through the fragment-growing strategy. By varying groups at the 3- and 6-positions of imidazo[1,2-a]pyridines, we studied the structure-activity relationships (SAR) profiles and identified a series of potent PI3Kα inhibitors. Representative derivatives showed good activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.