FT113 - FASN 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFT113Cat. No.: HY-111551CAS No.: 1630808-89-7分式: CHFNO分量: 409.41作靶点: Fatty Acid Synthase (FAS)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 62.5 mg/mL (152.6

2、6 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4425 mL 12.2127 mL 24.4254 mL5 mM 0.4885 mL 2.4425 mL 4.8851 mL10 mM 0.2443 mL 1.2213 mL 2.4425 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清

3、的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.08 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.08 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE

4、物活性 FT113种有效、可服的脂 酸合酶 (fatty acid synthase (FASN) 抑制剂，对全长重 组 FASN 酶的 IC50值为 213 nM。在 BT474 细胞中，FT113 抑制 FASN 的活性，IC50 值为 90 nM。FT113 具有抗增殖作，在体内和体外实验中，都具有抗癌作 1。IC50 & Target IC50: 213 nM (FASN), 90 nM (FASN, in BT474 cell) 1体外研究 FT113 shows anti-proliferative activity against PC3 and MV-411 cells wit

5、h IC50s of 47 and 26 nM,respectively 1.体内研究 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 man

6、ner in mice 1.REFERENCES1. Martin MW, et al. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN). Bioorg Med ChemLett. 2019 Apr 15;29(8):1001-1006.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820