35661-60-0|Fmoc-L-亮氨酸|Fmoc-Leu-OH，技术参数

1.Fmoc-L-亮氨酸产品物理参数：

2.Fmoc-L-亮氨酸同类产品列表：

3.Fmoc-L-亮氨酸物理化学性质：

4.Fmoc-L-亮氨酸急救措施：

① 必要的急救措施描述
吸入：如果吸入,请将患者移到新鲜空气处。 如果停止了呼吸,给于人工呼吸。
皮肤接触：用肥皂和大量的水冲洗。
眼睛接触：用水冲洗眼睛作为预防措施。
食入：切勿给失去知觉者从嘴里喂食任何东西。 用水漱口。
② 主要症状和影响，急性和迟发效应
据我们所知，此化学，物理和毒性性质尚未经完整的研究。
③ 及时的医疗处理和所需的特殊处理的说明和指示

5.Fmoc-L-亮氨酸消防措施：

① 灭火介质
灭火方法及灭火剂
用水雾,耐醇泡沫,干粉或二氧化碳灭火。
② 源于此物质或混合物的特别的危害
碳氧化物, 氮氧化物
③ 给消防员的建议
如必要的话,戴自给式呼吸器去救火。

6.Fmoc-L-亮氨酸泄露应急处理：

① 人员的预防,防护设备和紧急处理程序
防止粉尘的生成。 防止吸入蒸汽、气雾或气体。
② 环境保护措施
不要让产物进入下水道。
③ 抑制和清除溢出物的方法和材料
扫掉和铲掉。 存放进适当的闭口容器中待处理。

7.Fmoc-L-亮氨酸操作处置与储存：

① 安全操作的注意事项
在有粉尘生成的地方,提供合适的排风设备。
② 安全储存的条件,包括任何不兼容性
贮存在阴凉处。 容器保持紧闭，储存在干燥通风处。
建议的贮存温度： 2 - 8 °C

8.Fmoc-L-亮氨酸毒性和生态：

Fmoc-L-亮氨酸生态学数据:

对水是稍微有危害的不要让未稀释或大量的产品接触地下水、水道或者污水系统，若无政府许可，勿将材料排入周围环境。

9.Fmoc-L-亮氨酸安全信息：

10.Fmoc-L-亮氨酸海关：

11.Fmoc-L-亮氨酸文献：

Aspartate-modified doxorubicin on its N-terminal increases drug accumulation in LAT1-overexpressing tumors.

Weidang Wu, Yan Dong, Jing Gao, Min Gong, Xing Zhang, Weiling Kong, Yazhuo Li, Yong Zeng, Duanyun Si, Zihong Wei, Xiaoyan Ci, Lixin Jiang, Wei Li, Quansheng Li, Xiulin Yi, Changxiao Liu

文献索引：Cancer Sci. 106 , 747-56, (2015)

全文：HTML全文

摘要

L-type amino acid transporter 1 (LAT1), overexpressed on the membrane of various tumor cells, is a potential target for tumor-targeting therapy. This study aimed to develop a LAT1-mediated chemotherapeutic agent. We screened doxorubicin modified by seven different large neutral amino acids. The aspartate-modified doxorubicin (Asp-DOX) showed the highest affinity (Km = 41.423 μmol/L) to LAT1. Aspartate was attached to the N-terminal of DOX by the amide bond with a free carboxyl and a free amino group on the α-carbon atom of the Asp residue. The product Asp-DOX was characterized by HPLC/MS. In vitro, Asp-DOX exerted stronger inhibition on the cancer cells overexpressing LAT1 and the uptake of Asp-DOX was approximately 3.5-fold higher than that of DOX in HepG2 cells. Pharmacokinetic data also showed that Asp-DOX was expressed over a longer circulation time (t1/2 = 49.14 min) in the blood compared to DOX alone (t1/2 = 15.12 min). In HepG2 and HCT116 tumor-bearing mice, Asp-DOX achieved 3.1-fold and 6.4-fold accumulation of drugs in tumor tissue, respectively, than those of the unmodified DOX. More importantly, treatment of tumor-bearing mice with Asp-DOX showed a significantly stronger inhibition of tumor growth than mice treated with free DOX in HepG2 tumor models. Furthermore, after Asp modification, Asp-DOX avoided MDR mediated by P-glycoprotein. These results suggested that the Asp-DOX modified drug may provide a new treatment strategy for tumors that overexpress LAT1 and MDR1.© 2015 The Authors. Cancer Science published by Wiley Publishing Asia Pty Ltd on behalf of Japanese Cancer Association.

12.Fmoc-L-亮氨酸英文别名：