洛美曲索
| 中文名称 | 洛美曲索 |
|---|---|
| 中文同义词 | 洛美曲索;洛美曲索水合物;化合物 T15826 |
| 英文名称 | Lometrexol |
| 英文同义词 | Lometrexol;(6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic acid;N-[4-[2-[[(6R)-2-Amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid;N-[4-[2-[[(R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]pyrimidin]-6-yl]ethyl]benzoyl]-L-glutamic acid;L-Glutamic acid, N-(4-(2-((6R)-2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-;L-Glutamic acid, N-(4-(2-(2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-D)pyrimidin-6-yl)ethyl)benzoyl)-, (R)-;Lometrexolum;Lometrexolum [inn-latin] |
| CAS号 | 106400-81-1 |
| 分子式 | C21H25N5O6 |
| 分子量 | 443.45 |
| EINECS号 | |
| 相关类别 | Aromatics;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 106400-81-1.mol |
| 结构式 |  |
洛美曲索 性质
| 密度 | 1.56±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥5mg/mL |
| 酸度系数(pKa) | 3.60±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至浅黄色至浅橙色 |
| 稳定性 | 吸湿性 |
GARFT
Lometrexol hydrate (DDATHF hydrate) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides.
Lometrexol hydrate (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells.
Lometrexol hydrate (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells.
Lometrexol hydrate induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs).
Cell Viability Assay
| Cell Line: | Mouse leukemia L1210 cells |
| Concentration: | 1, 30 μM |
| Incubation Time: | 2, 4, 6, 8, 10 hours |
| Result: | Induced rapid and complete growth inhibition. |
Cell Cycle Analysis
| Cell Line: | L1210 cells |
| Concentration: | 1 μM |
| Incubation Time: | 2, 4, 8, 12, 24 hours |
| Result: | Caused a rapid loss of the G2/M phase population of cells and an early S phase accumulation of cells by 8 hours. By 24 h, the S phase population appeared to be slowly shifting to higher DNA content, and hence, from mid-to-late S phase. |
Lometrexol hydrate (DDATHF hydrate; i.p.; 15-60 mg/kg; on gestation day 7.5) increases the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Lometrexol hydrate (i.p.; 40 mg/kg) maximally inhibits GARFT activity after at 6 hours and thereafter gradually increases with time but remains significantly lower than control even at 96 hours. Levels of ATP, GTP, dATP and dGTP of NTDs embryonic brain tissue decreases significantly at 6 h, and more significantly over time.
| Animal Model: | C57BL/6 mice (7-8 week, 18-20 g) |
| Dosage: | 15, 30, 35, 40, 45 and 60 mg/kg |
| Administration: | Intraperitoneal injection; on gestation day 7.5 |
| Result: | Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-14521 | 洛美曲索 Lometrexol | 106400-81-1 | 1mg | 1000元 |
| 2024/01/25 | HY-14521B | 洛美曲索 Lometrexol hydrate | 1 mg | 2300元 |