Lometrexol (DDATHF) 是一种抗嘌呤抗叶酸剂,可抑制甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT) 的活性,但不会诱导可检测水平的 DNA 链断裂。洛美曲醇可进一步抑制嘌呤从头合成,导致细胞增殖和凋亡异常,甚至细胞周期停滞。洛美曲索具有抗癌活性。 Lometrexol 也是一种有效的人类丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。
Cas No. | 106400-81-1 |
别名 | 洛美曲索,DDATHF |
化学名 | N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid |
Canonical SMILES | O=C(N[C@H](C(O)=O)CCC(O)=O)C1=CC=C(CC[C@H]2CNC(N=C(N)NC3=O)=C3C2)C=C1 |
分子式 | C21H25N5O6 |
分子量 | 443.5 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Glycinamide ribonucleotide formyltransferase (GART) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexol is a folate analog antimetabolite with antineoplastic activity. At nanomolar conentrations, it inhibits GART preventing de novo purine synthesis, inhibiting DNA synthesis, arresting cells in the S phase of the cell cycle, and inhibiting tumor cell proliferation. |