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Lometrexol hydrate

CAS No. : 1435784-14-7

MCE 站：Lometrexol hydrate

产品活性：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。Lometrexol hydrate 还是一种有效的人丝氨酸羟甲基转移酶 1/2 (hSHMT1/2) 抑制剂。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Antifolate  |  Apoptosis

In Vitro: Lometrexol hydrate (DDATHF hydrate) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides.
Lometrexol hydrate (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells.
Lometrexol hydrate (1 μM; 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).

In Vivo: 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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