106400-81-1
基本信息
洛美曲索水合物
Lometrexol
Lometrexolum
LY 264618 hydrate
Lometrexol hydrate
Lometrexol(LY 264618)
Lometrexolum [inn-latin]
(6R)-5,10-Dideaza-5,6,7,8-tetrahydrofolic 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)-
物理化学性质
| 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 |
安全数据
| 危险性符号(GHS) |  GHS06 |
| 警示词 | 危险 |
| 危险性描述 | H301 |
| 防范说明 | P301+P310 |
| 危险品标志 | T |
| 危险类别码 | 25 |
| 安全说明 | 45 |
| 危险品运输编号 | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
常见问题列表
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. |