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106400-81-1

中文名称 洛美曲索
CAS 106400-81-1
分子式 C21H25N5O6
分子量 443.45
MOL 文件 106400-81-1.mol
更新日期 2023/03/20 15:41:25
106400-81-1 结构式 106400-81-1 结构式

基本信息

中文别名
洛美曲索
洛美曲索水合物
英文别名
LY 264618
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 Germany3
洛美曲索价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-14521洛美曲索
Lometrexol
106400-81-11mg1000元
2024/04/30HY-14521洛美曲索
Lometrexol
106400-81-110mM * 1mLin DMSO2750元
2024/04/30HY-14521洛美曲索
Lometrexol
106400-81-110 mg4000元

常见问题列表

生物活性
Lometrexol hydrate (DDATHF hydrate) 是一种抗嘌呤类抗叶酸 (antifolate) 药,可抑制甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 的活性,但不会引起可检测水平的 DNA 链断裂。Lometrexol hydrate 可以进一步抑制嘌呤从头合成,导致异常的细胞增殖,凋亡 (apoptosis) 和细胞周期停滞。Lometrexol hydrate 具有抗癌活性。Lometrexol hydrate 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。
靶点

GARFT

体外研究

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.
体内研究

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.
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