| Identification | Back Directory | [Name]
Methanone, [6-[[5-[3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl]-2-pyrazinyl]oxy]-1-methyl-1H-indol-2-yl][4-[[4-(2,2,2-trifluoroethoxy)phenyl]methyl]-1-piperazinyl]- | [CAS]
2591440-71-8 | [Synonyms]
Methanone, [6-[[5-[3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl]-2-pyrazinyl]oxy]-1-methyl-1H-indol-2-yl][4-[[4-(2,2,2-trifluoroethoxy)phenyl]methyl]-1-piperazinyl]- | [Molecular Formula]
C36H32F3N7O5 | [MOL File]
2591440-71-8.mol | [Molecular Weight]
699.68 |
| Hazard Information | Back Directory | [Uses]
STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model[1]. | [IC 50]
STAT3 | [References]
[1] Peng He, et al. Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment. J Med Chem. 2022 Nov 24;65(22):15487-15511. DOI:10.1021/acs.jmedchem.2c01554 |
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