产品说明书
LY 345899
 |
同义名 : | - |
| CAS号 : | 10538-99-5 | |
| 货号 : | A786224 | |
| 分子式 : | C20H21N7O7 | |
| 纯度 : | 99%+ | |
| 分子量 : | 471.423 | |
| MDL号 : | MFCD29920315 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 120 mg/mL(254.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MTHFD2 is a mitochondrial methylenetetrahydrofolate dehydrogenase and cyclohydrolase involved in one-carbon metabolism. It is responsible for the oxidation of methylene-THF to 10-formyl-THF in mitochondria, which is highly overexpressed in cancer cells and embryonic cells. LY345899, a Folate analog, is a MTHFD inbhibitor with IC50 values of 96 nM and 663 nM for MTHFD1 and MTHFD2, respectively[1]. LY345899 treatment for 72 hours caused a decrease in the cell viability of the CRC cells with highly expressed MTHFD2 (LoVo, SW620, HCT116). LY345899 (1 μM; 14 days) significantly reduced cell colony formation among these CRC cells. Further, LY345899 treatment decreased cellular NADPH/NADP+ and GSH/GSSG levels. Accordingly, LY345899 treatment for 48 hours obviously enhanced cell death under hypoxia or detached conditions. In SW620-based xenograft mice, LY345899 (5 mg/kg or 10 mg/kg; i.p.; 5 d/wk) showed potent antitumor activity in vivo, which was evident by the reduced SW620 cell or PDX-based tumor growth and tumor weight[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.61mL 2.12mL 1.06mL |
21.21mL 4.24mL 2.12mL |
| 参考文献 |
|---|