中文名称: | 洛美曲索水合物 | ||||
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英文名称: | Lometrexol hydrate | ||||
别名: | 洛美曲索水合物 DDATHF | ||||
CAS No: | 106400-81-1 | 分子式: | C21H25N5O6.XH2O | 分子量: | 443.45(anhydrous basis) |
CAS No: | 106400-81-1 | ||||
分子式: | C21H25N5O6.XH2O | ||||
分子量: | 443.45(anhydrous basis) |
基本信息
产品编号:L10335 |
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产品名称:Lometrexol hydrate |
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CAS: |
106400-81-1 |
储存条件 |
粉末 |
2-8℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
443.45 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
40mg/mL (86.68mM; Need ultrasonic and warming |
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Ethanol |
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Water |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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靶点/IC50 |
GARFT |
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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 |
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Cell Line: |
Mouse leukemia L1210 cells |
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Concentration: |
1, 30μM |
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Incubation Time: |
2, 4, 6, 8, 10 hours |
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Result: |
Induced rapid and complete growth inhibition. |
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Cell Cycle Analysis |
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Cell Line: |
L1210 cells |
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Concentration: |
1μM |
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Incubation Time: |
2, 4, 8, 12, 24 hours |
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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. |
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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. |
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Animal Model: |
C57BL/6 mice (7-8 week, 18-20 g) |
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Dosage: |
15, 30, 35, 40, 45 and 60mg/kg |
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Administration: |
Intraperitoneal injection; on gestation day 7.5 |
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Result: |
Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )