79640-70-3 甲氨蝶呤 α-叔丁酯

名称和标识

中文名: 甲氨蝶呤 α-叔丁酯
英文名: Methotrexate α-tert-Butyl Ester
CAS号: 79640-70-3
分子式: C24H30N8O5
分子量: 510.55
中文别名: (S)-5-(叔丁氧基)-4-(4-(((2,4-二氨基喋啶-6-基)甲基)(甲基)氨基)苯甲酰胺基)-5-氧代戊酸; 甲氨蝶呤伪-叔丁酯
英文别名: (S)-5-(tert-butoxy)-4-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)-5-oxopentanoic acid; L-Glutamic acid, N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-, 1-(1,1-dimethylethyl) ester; Methotrexate a-tert-Butyl Ester; Methotrexate Impurity 8; α-OtBu-MTX; (S)-2-{4-[(2,4-Diamino-pteridin-6-ylmethyl)-methyl-amino]-benzoylamino}-pentanedioic acid 1-tert-butyl ester; methotrexate-α-tert-butylester; methotrexate-α-OtBu; α-tert-butyl-N-[4-[[(2,4-diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamate; MTX-α-OtBu

用途与制备

生物活性 Methotrexate α-tert-butyl ester，经 OtBu 修饰，显著降低 HT1080 荷瘤小鼠的肿瘤生长。Methotrexate 是一种抗代谢和抗叶叶酸剂，也是一种免疫抑制剂和抗肿瘤药物。
体外研究 OtBu-MTX-PVG is less HT1080 than MTX-PVG against HT1080 cells. It shows that protection of the α-carboxyl group of MTX results in reduced in vitro activity.
体内研究 Lys-MTXcleavable- (OtBu) significantly reduces tumor growth in HT1080 tumor bearing mice. The protection of the α-carboxyl group of methotrexate may be used to improve the circulatory half-life and reduce the liver accumulation of similar MTX-conjugated dendrimers, while still retaining antitumor activity in vivo. Animal Model: Female, Balb/c nu/nu, 6 weeks (bearing HT1080 cells) Dosage: 30 mg/kg Administration: Once per week for 2 weeks Result: Showed a significant (63%) reduction in tumor size on day 12.

医药

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