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DOTA-?NHS-?ester

CAS No. : 170908-81-3

MCE 站：DOTA-?NHS-?ester

产品活性：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。

研究领域：Antibody-drug Conjugate/ADC Related

作用靶点：ADC Linker

In Vitro: 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 ⁶⁴Cu, ⁶⁴Cu-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.

In Vivo: In a microPET images of a mouse bearing SKOV3 tumor, ⁶⁴Cu-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.

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