79640-70-3
中文名稱
Methotrexate α-tert-Butyl Ester
CAS
79640-70-3
分子式
C24H30N8O5
更新日期
2024/11/05 14:08:10
基本信息
中文別名
187819 英文別名
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
常見問題列表
生物活性
Methotrexate α-tert-butyl ester，經(jīng) OtBu 修飾，顯著降低 HT1080 荷瘤小鼠的腫瘤生長(zhǎng)。Methotrexate 是一種抗代謝和抗葉葉酸劑，也是一種免疫抑制劑和抗腫瘤藥物。體外研究
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.
體內(nèi)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. |