| Description | FIDAS-5, a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM, competitively inhibits S-adenosylmethionine (SAM) binding to MAT2A. It exhibits anticancer activities. |
| In vitro | FIDAS-5可作为细胞周期抑制剂，抑制 p21WAF1/CIP1的表达。FIDAS-5（3 μM；36小时）处理降低了LS174T细胞中S-腺苷甲硫氨酸（SAM）和S-腺苷同型半胱氨酸（SAH）的水平。FIDAS-5（3 μM；7天；LS174T细胞）处理显著抑制LS174T细胞的增殖。FIDAS-5（3 μM）处理抑制LS174T结肠直肠癌细胞中c-Myc和cyclinD1的表达。 |
| In vivo | 小鼠连续一周每天通过口腔灌注的方式接受FIDAS-5（20 mg/kg）治疗后，肝脏中的SAM水平显著下降。同样，FIDAS-5（20 mg/kg；口腔灌注；每日；连续两周；无胸腺裸鼠）的治疗显著抑制了移植瘤的生长，同时对小鼠的体重影响微乎其微。 |
| Target activity | Mat2A:2.1 μM |
| molecular weight | 261.72 |
| Molecular formula | C15H13ClFN |
| CAS | 1391934-98-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 125 mg/mL (477.61 mM), Sonication is recommended. |
| References | 1. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803. |
| Citations | 1. He X C, Wang J, Shi M Y, et al.Hypoxia-induced one-carbon metabolic reprogramming in glioma stem-like cells.Life Medicine.2023: lnad048. |