Antibody-drug conjugates (ADCs) consist of a desirable monoclonal antibody, an active cytotoxic drug and an appropriate linker. An appropriate linker between the antibody and the cytotoxic drug provides a specific bridge, and thus helps the antibody to selectively deliver the cytotoxic drug to tumor cells and accurately releases the cytotoxic drug at tumor sites. In addition to conjugation, the linkers maintain ADCs’ stability during the preparation and storage stages of the ADCs and during the systemic circulation period.
The ADCs currently undergoing clinical evaluation contain linkers are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, such as reduction in the cytoplasm, exposure to acidic conditions in the lysosome, or cleavage by specific proteases within the cell. Noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule, which will retain the linker and the amino acid by which it was attached to the antibody.
The selection of linker is target dependent, based on the knowledge of the internalization and degradation of the antibody-target antigen complex, and a preclinical in vitro and in vivo activity comparison of conjugates. Moreover, the choice of a linker is also influenced by which cytotoxin is used, as each molecule has different chemical constraints, and frequently the drug structure lends itself to a specific linker.
| Cat. No. | Product Name | CAS No. | Purity | Chemical Structure |
|---|---|---|---|---|
| KM32664 | 11-Azidoundecanoic acid | 118162-45-1 | 99% |
|
| KM33208 | 12-Azido-dodecanoyl-OSu | 2489524-00-5 | ≥97% |
|
| KM35208 | 15-Azido-pentadecanoic acid | 118162-46-2 | 99% |
|
| KM35529 | 18-Azido-stearic acid | 1529763-58-3 | 95% |
|
| KM3190 |
2-Aminoethyl-mono-amide-DOTA-tris(tBu ester)
2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) 是用于肿瘤预靶向的大环 DOTA 衍生物。 |
173308-19-5 | ≥98% |
|
| KM38963 | 4-Azido-2,3,5,6-tetrafluorobenzoic Acid | 122590-77-6 | 98% |
|
| KM35289 | 6-Azido-hexylamine | 349553-73-7 | 98% |
|
| KM19299 |
6-Maleimidohexanoic acid N-hydroxysuccinimide ester
6-Maleimidohexanoic acid N-hydroxysuccinimide ester (EMCS) 是一种异双官能团交联剂。EMCS 是一种制备半抗原结合物和酶免疫偶联物的独特而有用的试剂。 |
55750-63-5 | 98% |
|
| KM37310 | 8-Azido-octanoyl-OSu | 2576471-56-0 |
|
|
| KM8687 |
Acid-PEG2-SS-PEG2-acid
Acid-PEG2-SS-PEG2-acid 是一种可降解 (cleavable) 的含 4 个单元 PEG 的 ADC linker，可用于合成抗体偶联药物 (ADC)。 |
1807539-10-1 | ≥95% |
|
| KM9876 |
Ald-Ph-amido-C2-nitrate
Ald-Ph-amido-C2-nitrate (Example XXIVb) 是一种不可降解 (non-cleavable) 的 ADC linker，可用于合成抗体偶联药物 (ADC)。 |
141534-26-1 | 98% |
|
| KM11529 |
Ald-Ph-amido-PEG1-C2-NHS ester
Ald-Ph-amido-PEG1-C2-NHS ester 是一种不可降解的含 1 个单元 PEG 的 linker，可用于合成抗体偶联药物 (ADC) 。 |
2101206-80-6 | 98% |
|
| KM10829 |
Ald-Ph-amido-PEG1-C2-Pfp ester
Ald-Ph-amido-PEG1-C2-Pfp ester 是 一种不可降解的含 1 个单元 PEG 的 linker，可用于合成抗体偶联药物 (ADC) 。 |
2101206-67-9 | 98% |
|
| KM5252 |
Ald-Ph-amido-PEG2
Ald-Ph-amido-PEG2 是一种不可降解 (non-cleavable) 的含 2 个单元 PEG 的 ADC linker，可用于合成抗体偶联药物 (ADC)。 |
1061569-06-9 | 98% |
|
| KM11528 |
Ald-Ph-amido-PEG2-C2-NHS ester
Ald-Ph-amido-PEG2-C2-NHS ester 是 一种不可降解的含 2 个单元 PEG 的 linker，可用于合成抗体偶联药物 (ADC) 。 |
1807521-07-8 | 98% |
|
| KM9479 |
Ald-Ph-amido-PEG2-C2-Pfp ester
Ald-Ph-amido-PEG2-C2-Pfp ester是 一种不可降解的含 2 个单元 PEG 的 linker，可用于合成抗体偶联药物 (ADC) 。 |
2101206-60-2 | 98% |
|
| KM11492 |
Ald-Ph-amido-PEG3-C-COOH
Ald-Ph-amido-PEG3-C-COOH 是用于抗体偶联药物 (ADC) 的不可降解 (non-cleavable) 的 linker。 |
1007215-91-9 | 98% |
|
| KM11527 |
Ald-Ph-amido-PEG3-C1-Boc
Ald-Ph-amido-PEG3-C1-Boc 是属于聚乙二醇 (PEG) 的一种 ADC linker。 |
1007215-94-2 | 98% |
|
| KM11383 |
Ald-Ph-amido-PEG3-C2-Pfp ester
Ald-Ph-amido-PEG3-C2-Pfp ester 是一种不可降解 (non-cleavable) 的含 3 个单元 PEG 的 ADC linker，可用于合成抗体偶联药物 (ADC)。 |
2101206-21-5 | 98% |
|
| KM11526 |
Ald-Ph-amido-PEG4-C2-acid
Ald-Ph-amido-PEG4-C2-acid 是用于抗体偶联药物 (ADC) 的不可降解 (non-cleavable) 的 linker。 |
1309460-27-2 | 98% |
|
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