FT113 |
| Katalog-Nr.GC64974 |
FT113 ist ein potenter und oral aktiver FettsÄuresynthase (FASN)-Hemmer mit einem IC50-Wert von 213 nM fÜr rekombinantes menschliches FASN-Enzym in voller LÄnge. In zellbasierten Assays blockiert FT113 die FASN-AktivitÄt in BT474-Zellen (IC50, 90 nM). FT113 zeigt antiproliferative AktivitÄt und weist sowohl in vitro als auch in vivo AntikrebsaktivitÄt auf.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1630808-89-7
Sample solution is provided at 25 µL, 10mM.
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FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo[1].
FT113 shows anti-proliferative activity against PC3 and MV-411 cells with IC50s of 47 and 26 nM, respectively[1].
FT113 (5 mg/kg, p.o.) exhibits potent oral bioavailability of 95% and 84% in mice and rats, respectively[1].FT113 (5, 25, or 50 mg/kg, p.o., twice daily for 16 days) increases malonyl-CoA concentration in tumors, inhibits tumor growth in a dose-dependent manner in mice[1].
[1]. Martin MW, et al. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN). Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006.
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