Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lometrexol (LY 264618) 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 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 具有抗癌活性。Lometrexol 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 721 | 现货 | ||
5 mg | ¥ 1,630 | 现货 | ||
10 mg | ¥ 2,380 | 现货 | ||
25 mg | ¥ 3,950 | 现货 | ||
50 mg | ¥ 5,630 | 现货 | ||
100 mg | ¥ 7,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,910 | 现货 |
产品描述 | Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor. |
体外活性 | Lometrexol binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides. Lometrexol (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells. Lometrexol (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells[3]. |
体内活性 | Lometrexol (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) induces neural tube defects (NTDs) by disturbing purine metabolism and increases the rate of embryonic resorption and growth retardation in a dose-dependent manner. Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and Changes of ATP, GTP, dATP and dGTP levels[1]. Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1]. |
别名 | LY 264618, DDATHF |
分子量 | 443.45 |
分子式 | C21H25N5O6 |
CAS No. | 106400-81-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 36mg/mL (81.2mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.255 mL | 11.2752 mL | 22.5505 mL | 56.3761 mL |
5 mM | 0.451 mL | 2.255 mL | 4.5101 mL | 11.2752 mL | |
10 mM | 0.2255 mL | 1.1275 mL | 2.255 mL | 5.6376 mL | |
20 mM | 0.1128 mL | 0.5638 mL | 1.1275 mL | 2.8188 mL | |
50 mM | 0.0451 mL | 0.2255 mL | 0.451 mL | 1.1275 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Lometrexol 106400-81-1 Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism DHFR LY 264618 LY264618 LY-264618 DDATHF Inhibitor inhibitor inhibit