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작성일 : 22-04-21
[Iris Biotech] Permanent Linkers, PEG-Based Spacer Molecules

 

Permanent Linkers, PEG-Based Spacer Molecules  

 

This class of linkers is considered non-cleavable, meaning linker cleavage and payload release do not

depend on the differential properties between plasma and cytoplasmic compartments. Instead, the release of

the cytotoxic drug is postulated to occur after internalization of the ADC via antigen-mediated endocytosis

and delivery to lysosomal compartments, where the antibody is degraded to the level of amino acids through

intracellular proteolytic degradation. This process releases a drug derivative, formed by the cytotoxic drug,

the linker, and the amino acid residue to which the linker was covalently attached.

The following section displays examples of hetero-bifunctional PEG-based spacer molecules. As payloads

are quite often rather hydrophobic, PEG fragments help to solubilize the linker-payload conjugate, which is

essential to perform successful conjugation onto the antibody. It further helps to increase the solubility in

physiological media and to improve the pharmacokinetic properties of the whole ADC construct.

 

H-O2Oc-OH

Chemical name:

 

[2-(2-aminoethoxy)ethoxy]acetic acid

Cas-no.:

 

134978-97-5

Formula:

 

C6H13NO4

Molecular weight:

 

163.17 g/mol

 

 

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H-O2Oc-OH*HCl

Chemical name:

 

8-amino-3,6-dioxaoctanoic acid hydrochloride O

Cas-no.:

 

134979-01-4

Formula:

 

C6H13NO4*HCI

Molecular weight:

 

163.17*36,45 g/mol

 

 

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H-O2Oc-OtBu*HCI

Chemical name:

 

[2-(2-aminoethoxy)ethoxy]acetic acid tert-butyl ester*HCl

Cas-no.:

 

2098500-69-5

Formula:

 

C10H21NO4*HCI

Molecular weight:

 

219.28*36,45 g/mol

 

 

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H-O2Oc-O2Oc-O2Oc-O2Oc-OH

Chemical name:

 

8-amino-3,6-dioxaoctanoic acid tetramer

Cas-no.:

 

N/A

Formula:

 

C24H46N4O13

Molecular weight:

 

598.64 g/mol

 

 

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H-O2Oc-O2Oc-OH

Chemical name:

 

17-Amino-10-oxo-3,6,12,15-tetraoxa-9-azaheptadecan-1-oic acid

Cas-no.:

 

1143516-05-5

Formula:

 

C12H24N2O7

Molecular weight:

 

308.33 g/mol

 

 

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Ordering informations

    

Catalog No.

Product Name

Size

PEG2420

H-O2Oc-OH

1, 5 & 25g

PEG7940

H-O2Oc-OH*HCl

1, 5, 25, 100 & 250g

PEG2430

H-O2Oc-OtBu*HCI

250, 500mg, 1, 5 & 25g

PEG8060

H-O2Oc-O2Oc-O2Oc-O2Oc-OH

100, 250, 500mg, 1 & 5g

PEG1221

H-O2Oc-O2Oc-OH

250, 500mg, 1, 5 , 25 & 100g

 

 

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