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编 号：F623226
分子式：C21H27N5O7
分子量：461.47
分子式：C21H27N5O7
分子量：461.47
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是否有货
1mg
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CAS No: 1435784-14-7
产品详情
生物活性：
Lometrexol (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. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
体内研究：
Lometrexol (DDATHF；腹腔注射；15-60 mg/kg；在妊娠第 7.5 天) hydrate 通过干扰嘌呤代谢诱导神经管缺陷 (NTD)，并以剂量依赖的方式增加胚胎吸收率和生长迟缓。 Lometrexol (ip；40 mg/kg；在妊娠第 7.5 天) hydrate 降低甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 活性和 ATP、GTP、dATP 和 dGTP 水平的变化。 Lometrexol (腹腔注射；40 mg/kg；妊娠7.5天) hydrate 诱导神经管缺陷 (NTDs) 异常增殖和凋亡。Animal Model:C57BL/6 mice (7-8 week, 18-20 g)
Dosage:15, 30, 35, 40, 45 and 60 mg/kg
Administration:Intraperitoneal injection; on gestation day 7.5
Result:Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Animal Model:C57BL/6 mice (7-8 week, 18-20 g)
Dosage:40 mg/kg
Administration:Intraperitoneal injection; on gestation day 7.5
Result:Inhibited glycinamide ribonucleotide formyl transferase (GARFT) activity and GARFT activity was maximally inhibited after at 6 hours.Decreased the levels of ATP, GTP, dATP, and dGTP of NTDs embryonic brain tissue significantly at 6 hours.
Animal Model:C57BL/6 mice (7-8 week, 18-20 g)
Dosage:40 mg/kg
Administration:Intraperitoneal injection; on gestation day 7.5, for 4 days
Result:Decreased the expression of proliferation-related genes (Pcna, Foxg1 and Ptch1) and increased the expression of apoptosis-related genes (Bax, Casp8 and Casp9) in NTD groups.
体外研究：
Lometrexol (DDATHF) hydrate 与 GART 紧密结合，导致细胞内嘌呤核糖核苷酸快速和长时间消耗。Lometrexol (1-30 μM；2-10 小时) hydrate 诱导L1210 细胞的快速和完全生长抑制。 Lometrexol (1 μM；2-24 小时) hydrate 诱导小鼠白血病 L1210 细胞的细胞周期停滞。
Lometrexol (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. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
体内研究：
Lometrexol (DDATHF；腹腔注射；15-60 mg/kg；在妊娠第 7.5 天) hydrate 通过干扰嘌呤代谢诱导神经管缺陷 (NTD)，并以剂量依赖的方式增加胚胎吸收率和生长迟缓。 Lometrexol (ip；40 mg/kg；在妊娠第 7.5 天) hydrate 降低甘氨酰胺核糖核苷酸甲酰基转移酶 (GARFT) 活性和 ATP、GTP、dATP 和 dGTP 水平的变化。 Lometrexol (腹腔注射；40 mg/kg；妊娠7.5天) hydrate 诱导神经管缺陷 (NTDs) 异常增殖和凋亡。Animal Model:C57BL/6 mice (7-8 week, 18-20 g)
Dosage:15, 30, 35, 40, 45 and 60 mg/kg
Administration:Intraperitoneal injection; on gestation day 7.5
Result:Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Animal Model:C57BL/6 mice (7-8 week, 18-20 g)
Dosage:40 mg/kg
Administration:Intraperitoneal injection; on gestation day 7.5
Result:Inhibited glycinamide ribonucleotide formyl transferase (GARFT) activity and GARFT activity was maximally inhibited after at 6 hours.Decreased the levels of ATP, GTP, dATP, and dGTP of NTDs embryonic brain tissue significantly at 6 hours.
Animal Model:C57BL/6 mice (7-8 week, 18-20 g)
Dosage:40 mg/kg
Administration:Intraperitoneal injection; on gestation day 7.5, for 4 days
Result:Decreased the expression of proliferation-related genes (Pcna, Foxg1 and Ptch1) and increased the expression of apoptosis-related genes (Bax, Casp8 and Casp9) in NTD groups.
体外研究：
Lometrexol (DDATHF) hydrate 与 GART 紧密结合，导致细胞内嘌呤核糖核苷酸快速和长时间消耗。Lometrexol (1-30 μM；2-10 小时) hydrate 诱导L1210 细胞的快速和完全生长抑制。 Lometrexol (1 μM；2-24 小时) hydrate 诱导小鼠白血病 L1210 细胞的细胞周期停滞。
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