1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸 1-(2,5-二氧代-1-吡咯烷基)酯

中文名称:

1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸 1-(2,5-二氧代-1-吡咯烷基)酯

中文同义词:

1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸 1-(2,5-二氧代-1-吡咯烷基)酯;DOTA单-N-羟基琥珀酰亚胺酯;1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸 1-(2,5-二氧代-1-吡咯烷基)酯;DOTA-NHS ESTER,羟基琥珀酰亚胺-四氮杂环十二烷四乙酸

英文名称:

1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid, 1-(2,5-dioxo-1-pyrrolidinyl) ester

英文同义词:

1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid, 1-(2,5-dioxo-1-pyrrolidinyl) ester;DOTA-NHS-ester(B-280);DOTA mono-N-hydroxysuccinimide ester;DOTA-NHS-ester;1, 4, 7, 10-Tetraazacyclododecana-1, 4, 7-tris-tert-butyl acetate-10-N-a-Fmoc-N-e-acetamido-L-lysine);DOTA mono-NHS ester

CAS号:

170908-81-3

分子式:

C20H31N5O10

分子量:

501.49

EINECS号:

相关类别:

氨基酸衍生物;放射显影多肽产品;基准试剂

Mol文件:

170908-81-3.mol

沸点 

743.7±70.0 °C(Predicted)

密度 

1.51±0.1 g/cm3(Predicted)

酸度系数(pKa)

2.46±0.10(Predicted)

CAS 数据库

170908-81-3

生物活性

DOTA-NHS-ester 是用于 affibody 分子的交联剂 (linker)，可用于小型动物正电子发射断层扫描 (PET)，单光子发射计算机断层扫描 (SPECT) 和 CT 扫描。DOTA-NHS-ester 可用于标记放射研究剂或者成像探针以检测肿瘤。

体外研究

DOTA-NHS-ester can be used to modify human serum albumin (HSA) to produce DOTA-HSA. And DOTA-HSA is furtherly modified by Sulfo-SMCC (HY-D0975) to obtain DOTA-HSA-SMCC. DOTA-HSA-SMCC is conjugated to ZHER2:342 and the final product is DOTA-HSA-Z HER2 :342 . In a cell uptake assay, DOTA-HSA-Z HER2 :342 is labeled by 64 Cu, 64 Cu-DOTA-HSA-Z HER2 :342 (0.5-2 hours) slowly accumulates in the SKOV3 cells and reaches 0.71% of the applied activity at 0.5 h and the uptake increased to 1.58% at 2 h.

体内研究

In a microPET images of a mouse bearing SKOV3 tumor, 64 Cu-DOTA-HSA-Z HER2 :342 is injected to the mouse tail. microPET images of a mouse bearing SKOV3 tumor at 1, 4, 24 and 48 h after tail vein injection.The SKOV3 tumor is visible with a low tumor-to-background contrast at 1 h post-injection (p.i.), but with a very good tumor-to-background contrast at 4 and 24 h p.i.Quantification analysis reveals that the SKOV3 tumor uptake values increases with time and are found to be 5.63%, 9.98%, 14.34% and 14.12% ID/g at 1, 4, 24, and 48 h, respectively.