For research use only. Not for therapeutic Use.
HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC50=27.8 nM; ATP inhibition: IC50=24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis[1].
HP590 (0-40 μM; 72 h) shows anti-proliferative activities to MKN45, AGS, and MGC803 cells[1].
HP590 (0-40 nM; 0-24 h) inhibits STAT3 Tyr705 and Ser727 phosphorylation in GC cells, blocks the expression of STAT3 downstream genes (c-Myc and cyclin D1) in GC cells, reduces IL-6-mediated STAT3 nuclear translocation in MKN45 cells[1].
HP590 (5-20 nM; 48 h) induces gastric cancer cell apoptosis[1].
HP590 (oral administration; 25 and 50 mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model[1].
| Catalog Number | I042708 |
| CAS Number | 2971855-37-3 |
| Synonyms | [4-[[4-(2,2,2-trifluoroethoxy)phenyl]methyl]piperazin-1-yl]-[4-[3-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]phenyl]methanone |
| Molecular Formula | C29H24F6N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H24F6N4O3/c30-28(31,32)18-41-24-11-1-19(2-12-24)17-38-13-15-39(16-14-38)27(40)22-5-3-21(4-6-22)26-36-25(37-42-26)20-7-9-23(10-8-20)29(33,34)35/h1-12H,13-18H2 |
| InChIKey | VFBJWQHKJOGQRX-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1CC2=CC=C(C=C2)OCC(F)(F)F)C(=O)C3=CC=C(C=C3)C4=NC(=NO4)C5=CC=C(C=C5)C(F)(F)F |
| Reference | [1]. He P, et al. Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr705/Ser727 Inhibitory Activity for Gastric Cancer Treatment. J Med Chem. 2022 Sep 14. |
