LY 345899)
| 中文名称 | LY 345899) |
|---|---|
| 中文同义词 | 化合物LY 345899;(2S)-2-(4-(3-氨基-1,9-二氧代-1,2,5,6,6A,7-六氢咪唑并[1,5-F]蝶啶-8(9H)-基)苯甲酰胺基)戊二酸 |
| 英文名称 | LY 345899) |
| 英文同义词 | 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]-;(2S)-2-(4-(3-Amino-1,9-dioxo-1,2,5,6,6a,7-hexahydroimidazo[1,5-f]pteridin-8(9H)-yl)benzamido)pentanedioic acid;inhibit,LY345899,LY-345899,Inhibitor,LY 345899,Methylenetetrahydrofolate Dehydrogenase (MTHFD) |
| CAS号 | 10538-99-5 |
| 分子式 | C20H21N7O7 |
| 分子量 | 471.42 |
| EINECS号 | |
| 相关类别 | 抑制剂 |
| Mol文件 | 10538-99-5.mol |
| 结构式 |  |
LY 345899) 性质
| 密度 | 1.82±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO:125.0(最大浓度 mg/mL);265.16(最大浓度 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | 3.46±0.10(Predicted) |
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。
Ki: 18 nM (MTHFD1); IC50: 96 nM (MTHFD1) and 663 nM (MTHFD2)
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.
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-101943 | LY 345899 | 1 mg | 1725元 | |
| 2024/04/30 | HY-101943 | LY 345899) LY 345899 | 10538-99-5 | 5mg | 4338元 |