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Lometrexol
产品编号 T15826Cas号 106400-81-1
别名 洛美曲索, LY 264618, DDATHF
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。
Lometrexol
产品编号 T15826 别名 洛美曲索, LY 264618, DDATHFCas号 106400-81-1
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 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 712 | 现货 | |
| 5 mg | ¥ 1,590 | 现货 | |
| 10 mg | ¥ 2,360 | 现货 | |
| 25 mg | ¥ 3,930 | 现货 | |
| 50 mg | ¥ 5,580 | 现货 | |
| 100 mg | ¥ 7,580 | 现货 | |
| 200 mg | ¥ 9,870 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 1,770 | 现货 |
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生物活性
化学信息
| 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 | 洛美曲索, LY 264618, DDATHF |
| 分子量 | 443.45 |
| 分子式 | C21H25N5O6 |
| CAS No. | 106400-81-1 |
储存&溶解度
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | 5% DMSO+40% PEG300+5% Tween 80+50% Saline: 5 mg/mL (11.28 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.  DMSO: 100 mg/ml (225.50 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
5% DMSO+40% PEG300+5% Tween 80+50% Saline/DMSO
DMSO
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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 ， 
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