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葡醛酸三甲曲沙

葡醛酸三甲曲沙用途

三甲氧基葡萄糖醛酸盐(NSC 352122)是一种叶酸拮抗剂。三甲氧基葡萄糖醛酸盐通过抑制二氢叶酸还原酶和阻止嘌呤核苷酸和胸苷酸的合成而影响DNA和RNA合成。葡萄糖醛酸三甲氧酯具有潜在的抗肿瘤活性[1]。

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葡醛酸三甲曲沙名称

[ CAS 号 ]:
82952-64-5

[ 中文名 ]:
葡醛酸三甲曲沙

[ 英文名 ]:
Trimetrexate glucuronate

[中文别名 ]:

三甲曲沙葡糖醛酸酯

[英文别名 ]:

CI 898 dihydrochloride
CI 898 TRIHYDROCHLORIDE
Trimetrexate glucuronate

葡醛酸三甲曲沙生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 叶酸

[体外研究]

三甲基苯甲酸葡萄糖醛酸盐(0.05-1μM 6 h)导致腺苷和鸟嘌呤酸减少,并以剂量依赖性方式显著增加WI-L2人淋巴母细胞的嘧啶核苷酸,如CTP、UTP[1]。三甲基苯甲酸葡萄糖醛酸盐(1μM,2小时)可将dTTP水平降低29%,还可降低dGTP和dATP,同时广泛抑制L1210小鼠白血病细胞中脱氧尿苷掺入DNA[1]。

[体内研究]

葡萄糖醛酸三甲氧酯(i.p.,100-225 mg/kg,每日,第1、5、9天)对患有L1210白血病的近交DBA/2小鼠具有抗肿瘤活性[1]。动物模型：L1210白血病的近交DBA/2小鼠[1]剂量：100、150、225 mg/kg给药：腹腔注射；每日的第1天、第5天和第9天结果：显示最大寿命T/C值为171%。动物模型：C57BL/6小鼠,具有M5076肿瘤[1]剂量：38,62 mg/kg给药：腹腔注射；每日的1-9天结果：高剂量62 mg/kg时显示毒性(>10%的早期死亡),低剂量38 mg/kg则显示无活性(寿命T/C<130%)。

[参考文献]

[1]. R C Jackson, et al. Biochemical pharmacology of the lipophilic antifolate, trimetrexate. Adv Enzyme Regul. 1984;22:187-206.

葡醛酸三甲曲沙物理化学性质

[ 密度 ]:
1.305 g/cm3

[ 沸点 ]:
647ºC at 760 mmHg

[ 分子式 ]:
C₂₅H₃₃N₅O₁₀

[ 分子量 ]:
563.55700

[ 闪点 ]:
345.1ºC

[ 精确质量 ]:
563.22300

[ PSA ]:
244.99000

[ LogP ]:
0.84680

葡醛酸三甲曲沙毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: LZ8945000

CAS REGISTRY NUMBER :: 82952-64-5

LAST UPDATED :: 199412

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C19-H23-N5-O3.C6-H10-O7

MOLECULAR WEIGHT :: 563.63

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 2027 ug/kg

TOXIC EFFECTS :: Vascular - BP lowering not characterized in autonomic section Gastrointestinal - other changes Blood - thrombocytopenia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 4054 mg/kg/3W-I

TOXIC EFFECTS :: Blood - changes in bone marrow (not otherwise specified)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 50 mg/kg/5D-C

TOXIC EFFECTS :: Blood - changes in leukocyte (WBC) count Blood - changes in platelet count Related to Chronic Data - changes in testicular weight

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Rodent - mouse Leukocyte

DOSE/DURATION :: 500 nmol/L

REFERENCE :: BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 40,1981,1990