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Details

Stereochemistry ACHIRAL
Molecular Formula C21H18N4O4S
Molecular Weight 422.457
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of HS-173

SMILES

CCOC(=O)C1=CN=C2C=CC(=CN12)C3=CC(NS(=O)(=O)C4=CC=CC=C4)=CN=C3

InChI

InChIKey=SEKOTFCHZNXZMM-UHFFFAOYSA-N
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

HIDE SMILES / InChI
Molecular Formula C21H18N4O4S
Molecular Weight 422.457
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27793006

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM. 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.

Originator

Korea Advanced Institute of Science and Technology
1
Curator's Comment: Lee H. et al, Korea Advanced Institute of Science and Technology, Korea.

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 0.8 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Preclinical
Unknown

Approved Use

Unknown
Primary
Preclinical
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.
2011 Apr 14
HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer.
2016 Nov 22
Patents

Patents

WO2016025656A1
3

Sample Use Guides

In Vivo Use Guide
Mice: In xenograft and orthotopic pancreatic tumor models, mice were treated by HS-173 intraperitoneally at a dose of 10 mg/kg
Route of Administration: Intraperitoneal
In Vitro Use Guide
When pancreatic cancer cells were treated with various concentrations (0.1- 10 uM) of HS-173, it reduced the cell viability in a dose and time-dependent manner. In particular, 1 uM of HS-173 inhibited the cell growth by 40-50% in Miapaca-2 and Aspc-1 cells at 48 h.
Substance Class Chemical
Created
by admin
on Sat Dec 16 18:08:59 UTC 2023
Edited
by admin
on Sat Dec 16 18:08:59 UTC 2023
Record UNII
2758X982JL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
HS-173
Code English
IMIDAZO(1,2-A)PYRIDINE-3-CARBOXYLIC ACID, 6-(5-((PHENYLSULFONYL)AMINO)-3-PYRIDINYL)-, ETHYL ESTER
Systematic Name English
Code System Code Type Description
CAS
1276110-06-5
Created by admin on Sat Dec 16 18:08:59 UTC 2023 , Edited by admin on Sat Dec 16 18:08:59 UTC 2023
PRIMARY
PUBCHEM
52936849
Created by admin on Sat Dec 16 18:08:59 UTC 2023 , Edited by admin on Sat Dec 16 18:08:59 UTC 2023
PRIMARY
FDA UNII
2758X982JL
Created by admin on Sat Dec 16 18:08:59 UTC 2023 , Edited by admin on Sat Dec 16 18:08:59 UTC 2023
PRIMARY
Related Record Type Details
PHOSPHATIDYLINOSITOL 4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT ALPHA ISOFORM
TARGET -> INHIBITOR
IC50
Related Record Type Details
Structure of HS-173
ACTIVE MOIETY
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