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。
货号:ajcx17364
CAS:1435784-14-7
分子式:C21H27N5O7
分子量：461.47
溶解度:DMF: 5 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity[1][2].

[1]. Xu L, et al. The effect of inhibiting glycinamide ribonucleotide formyl transferase on the development of neural tube in mice. Nutr Metab (Lond). 2016 Aug 23;13(1):56. [2]. Julie L Bronder, et al. Antifolates Targeting Purine Synthesis Allow Entry of Tumor Cells Into S Phase Regardless of p53 Function. Cancer Res. 2002 Sep 15;62(18):5236-41.