79640-70-3
中文名称
Methotrexate α-tert-Butyl Ester
CAS
79640-70-3
分子式
C24H30N8O5
更新日期
2024/10/07 18:32:32
基本信息
中文别名
187819 英文别名
Methotrexate α-tert-Butyl Ester(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
常见问题列表
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. |