DOTA-NHS-ester

Names

[ Name ]:
DOTA-NHS-ester

[Synonym ]:
1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid, 1-(2,5-dioxo-1-pyrrolidinyl) ester
1,4,7,10-Tetraazacyclododecane-1,4,7-triacetic acid,10-[2-[(2,5-dioxo-1-pyrrolidinyl)oxy]-2-oxoethyl]-
1,4,7,10-Tetraazacyclododecane-1,4,7,10-tetraacetic acid,1-(2,5-dioxo-1-pyrrolidinyl) ester

Biological Activity

[Description]:

DOTA-NHS-ester is a linker for affibody molecules and is applied in small animals PET, SPECT, and CT. DOTA-NHS-ester can be used to label radiotherapeutic agents or imaging probes for the detection of tumors[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Antibody-drug Conjugate >> 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-ZHER2:342[1]. In a cell uptake assay, DOTA-HSA-ZHER2:342 is labeled by 64Cu, 64Cu-DOTA-HSA-ZHER2:342 (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[1].

[In Vivo]

In a microPET images of a mouse bearing SKOV3 tumor, 64Cu-DOTA-HSA-ZHER2:342 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[1].

[References]

[1]. Hoppmann S, et al. Radiolabeled affibody-albumin bioconjugates for HER2-positive cancer targeting.Bioconjug Chem. 2011 Mar 16;22(3):413-2

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₃₁N₅O₁₀

[ Molecular Weight ]:
501.48800

[ Exact Mass ]:
501.20700

[ PSA ]:
188.54000

Safety Information

[ Hazard Codes ]:
Xn

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

DOTA-​NHS-​ester