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
SMILES
CCOC(=O)C1=CN=C2C=CC(=CN12)C3=CN=CC(NS(=O)(=O)C4=CC=CC=C4)=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
| 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 |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/21388141 | https://www.ncbi.nlm.nih.gov/pubmed/22929971Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27793006
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21388141 | https://www.ncbi.nlm.nih.gov/pubmed/22929971
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21388141 | https://www.ncbi.nlm.nih.gov/pubmed/22929971
Curator's Comment: Lee H. et al, Korea Advanced Institute of Science and Technology, Korea.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| HS-173, a novel PI3K inhibitor suppresses EMT and metastasis in pancreatic cancer. | 2016-11-22 |
|
| HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis. | 2013-01-01 |
|
| Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis. | 2011-04-14 |
Patents
Sample Use Guides
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
| Substance Class |
Chemical
Created
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admin
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Wed Apr 02 10:17:11 GMT 2025
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Wed Apr 02 10:17:11 GMT 2025
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| Record UNII |
2758X982JL
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| Record Status |
Validated (UNII)
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