| Bioactivity | STAT3-IN-25 (compound 4c) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-25 has luciferase activities IC50 of 5.3 nM and ATP inhibition IC50 of 4.2 nM.STAT3-IN-25 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 in the low nanomolar range by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-25 exhibits significant suppressive effects in a pancreatic cancer xenograft model[1]. | ||||||||||||
| CAS | 2591440-75-2 | ||||||||||||
| Formula | C36H29F6N7O4 | ||||||||||||
| Molar Mass | 737.65 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |
STAT3-IN-25
CAS: 2591440-75-2 F: C36H29F6N7O4 W: 737.65
STAT3-IN-25 (compound 4c) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tet
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