产品
编 号：F025386
分子式：C21H25N5O6
分子量：443.45
分子式：C21H25N5O6
分子量：443.45
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是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 106400-81-1
产品详情
生物活性：
Lometrexol (DDATHF), 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.
体内研究：
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.Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs).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, for 0, 6, 24, 48 and 96 hours
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) 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.
Lometrexol (DDATHF), 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.
体内研究：
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.Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs).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, for 0, 6, 24, 48 and 96 hours
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) 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.
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