Trimetrexate glucuronate

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

82952-64-5

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

CI-898 glucuronate

产品介绍

Trimetrexate glucuronate (NSC 352122) 是一种叶酸拮抗剂，可以抑制二氢叶酸还原酶 (dihydrofolate reductase)，从而阻止嘌呤核苷酸和胸苷酸的合成，影响 DNA 和 RNA 合成。具有潜在的抗肿瘤活性, 也可用于抑制肺孢子菌肺炎。

生物活性

Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibitingdihydrofolate reductaseand preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibitPneumocystis carinii pneumonia^[1]^[2].

体外研究
(In Vitro)

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^[1].
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^[1].

体内研究
(In Vivo)

Trimetrexate glucuronate (i.p., 100-225 mg/kg, daily, day 1, 5, 9) has antitumor activity in inbred DBA/2 mice with L1210 leukemia^[1].

Animal Model:	Inbred DBA/2 mice with L1210 leukemia^[1]
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^[1]
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.

Clinical Trial

分子量

563.56

Formula

C₂₅H₃₃N₅O₁₀

CAS 号

82952-64-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.