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洛美曲索水合物  99.56%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（≥5mg/mL）
产品描述：基本信息 产品编号：L10335 产品名称：Lometrexol hydrate CAS: 106400-81-1   储存条件 粉末 2-8℃ 四年     分子式： C21H25N5O6.XH2O 溶于液体 -80℃ 六个月 分子量 443.45 -20℃ 一个月 化学名：  (2S)-2-[[4-[2-[(6R)-2-amino-4-oxo-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]amino]pentanedioic acid   Solubility (25°C)   体外 DMSO 40mg/mL (86.68mM; Need ultrasonic and warming Ethanol   Water   体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.1670mL 10.8349mL 21.6699mL 5mM 0.4334mL 2.1670mL 4.3340mL 10mM 0.2167mL 1.0835mL 2.1670mL   生物活性 产品描述 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。 靶点/IC50 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 (1-30μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells . Lometrexol hydrate (1μM; 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, 30μM Incubation Time: 2, 4, 6, 8, 10 hours Result: Induced rapid and complete growth inhibition. Cell Cycle Analysis Cell Line: L1210 cells Concentration: 1μM 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 60mg/kg Administration: Intraperitoneal injection; on gestation day 7.5 Result: Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
保存条件：2-8℃

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