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DOTA-NHS-ester£¬IC-0172809
Click£º1991     Release date£º2013-5-10    Author£ºAdministrator    Source£ºOriginal

DOTA-NHS-ester,

170908-81-3

 

 

 

Cat.No.:

IC-0172809

 

 

 

Product Information

Biological Activity

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].
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 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 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].

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species

Mouse

Rat

Rabbit

Guinea pig

Hamster

Dog

Weight (kg)

0.02

0.15

1.8

0.4

0.08

10

Body Surface Area (m2)

0.007

0.025

0.15

0.05

0.02

0.5

Km factor

3

6

12

8

5

20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by  (Animal B Km / Animal A Km)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Order Information

 

Quantity

Price($)

Price($)

Availability

5mg

$300.00

€330.00

In stock

10mg

$400.00

€440.00

In stock

50mg

$900.00

€990.00

In stock

Free Delivery on orders over $350.00.

Chemical Information

Molecular Weight

501.49

Formula

 C20H31N5O10

CAS Number

170908-81-3

Purity

>98%

 

 

 

 

 

Solubility

DMSO: 50 mg/mL (99.70 mM)

Storage

 at -20¡ãC

 

 

 

 

 

Reference

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

 

 

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