10538-99-5
中文名称
LY 345899)
英文名称
LY 345899)
CAS
10538-99-5
分子式
C20H21N7O7
分子量
471.42
MOL 文件
10538-99-5.mol
更新日期
2024/07/12 16:05:25
10538-99-5 结构式
基本信息
中文别名
化合物LY 345899 英文别名
LY 345899)LY-345899 (LY345899
L-Glutamic acid, N-[4-(3-amino-1,2,5,6,6a,7-hexahydro-1,9-dioxoimidazo[1,5-f]pteridin-8(9H)-yl)benzoyl]-
物理化学性质
密度1.82±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO:125.0(Max Conc. mg/mL);265.16(Max Conc. mM)
酸度系数(pKa)3.46±0.10(Predicted)
形态固体
颜色Light yellow to yellow
常见问题列表
生物活性
LY 345899 是一种叶酸的类似物，也是一种亚甲基四氢叶酸脱氢酶 (MTHFD1; DC301) 和 MTHFD2 抑制剂，其 IC50 值分别为 96 nM 和 663 nM，对 MTHFD1 的 Ki 值为 18 nM。靶点
Ki: 18 nM (MTHFD1); IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2)
体外研究
LY 345899 could suppress the MTHFD enzyme in the cytoplasm and mitochondria.
LY 345899 could disturb the NADPH and redox homeostases and accelerate cell death under oxidative stress, such as hypoxia, or causing in vitro anchorage independence and in vivo impaired tumor growth and metastasis.
体内研究
LY345899 (Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks) shows potent antitumor activity and displays therapeutic activity against CRC in vivo .
| Animal Model: | SW620 or PDX-based BABL/c nude colorectal cancer (CRC) model |
| Dosage: | 5-10 mg/kg |
| Administration: | Intraperitoneal injection; 5-10 mg/kg; 5 d/wk; 4 weeks |
| Result: | Displayed lower cell proliferation indices and higher cell apoptosis.Exhibited no statistically significant weight loss or other signs of acute or delayed toxicity in mice. |