10538-99-5
中文名稱
LY 345899)
英文名稱
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
2024/10/25 16:41:16
10538-99-5 結(jié)構(gòu)式
基本信息
中文別名
化合物L(fēng)Y 345899 英文別名
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]-
物理化學(xué)性質(zhì)
密度1.82±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO:125.0(Max Conc. mg/mL);265.16(Max Conc. mM)
酸度系數(shù)(pKa)3.46±0.10(Predicted)
形態(tài)固體
顏色Light yellow to yellow
常見問題列表
生物活性
LY 345899 是一種葉酸的類似物，也是一種亞甲基四氫葉酸脫氫酶 (MTHFD1; DC301) 和 MTHFD2 抑制劑，其 IC50 值分別為 96 nM 和 663 nM，對 MTHFD1 的 Ki 值為 18 nM。靶點(diǎn)
Ki: 18 nM (MTHFD1); IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2)
體外研究
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.
體內(nèi)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. |