产品
编 号:F471695
分子式:C25H33N5O10
分子量:563.56
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规格
价格
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5mg
询价
询价
10mg
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产品详情
生物活性:
Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia.

体内研究:
Trimetrexate glucuronate (i.p., 100-225 mg/kg, daily, day 1, 5, 9) has antitumor activity in inbred DBA/2 mice with L1210 leukemia.Animal Model:Inbred DBA/2 mice with L1210 leukemia
Dosage:100, 150, 225 mg/kg
Administration:Intraperitoneal injection; daily; day 1, 5, 9
Result:Showed the maximum lifespan T/C value of 171%.
Animal Model:C57BL/6 mice with M5076 tumor
Dosage:38, 62 mg/kg
Administration:Intraperitoneal injection; daily; 1-9 days
Result:Showed toxic (>10% early deaths) at high dose of 62 mg/kg and inactive (Lifespan T/C <130%) at lower dose of 38 mg/kg.

体外研究:
Trimetrexate glucuronate (0.05-1 μM 6 h) results in a decrease in adenosine and guanosine acids and a significant increase in the pyrimidine nucleotide such as CTP, UTP of WI-L2 human lymphoblastoid cells in a dose-dependent manner.Trimetrexate glucuronate (1 μM, 2 h) can reduce the level of dTTP by 29%, also decrease in the dGTP and dATP, while cause extensive inhibition of deoxyuridine incorporation into DNA in L1210 mouse leukemia cells.
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