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 |
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KM20334 | NO2-SPDMV | 663598-98-9 |
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KM4313 |
NO2-SPP-sulfo-Me
NO2-SPP-sulfo-Me 是一种用于制备抗体偶联药物 (ADC) 的可降解 linker 。 |
890409-87-7 |
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KM7929 |
PDB-Pfp
PDB-Pfp 是一种可降解的 ADC linker,用于抗体偶联药物 (ADCs) 的合成。 |
2088570-81-2 |
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KM11496 |
PDdB-Pfp
PDdB-Pfp 是一种可切割的 ADC Linker,用于靶向 TM4SF1 细胞外环 1 (ECL1) 的药物。 |
2101206-44-2 |
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KM3203 |
PDdEC-NB
PDdEC-NB 是一种谷胱甘肽可降解 (cleavable) 的 linker,用于抗体偶联药物 (ADC)。 |
1956318-90-3 |
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KM7021 |
PDEC-NB
PDEC-NB 是一种二硫键可降解 (cleavable) 的 linker,用于抗体偶联药物 (ADC)。 |
874302-76-8 | 98% |
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KM8548 |
PDP-C1-Ph-Val-Cit
PDP-C1-Ph-Val-Cit 是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联药物 (ADC)。 |
1610769-13-5 |
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KM10689 |
PDP-Pfp
PDP-Pfp 是一种可还原的 ADC Linker,用于靶向 TM4SF1 细胞外环 1 (ECL1) 的药物。 |
160580-70-1 | 98% |
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KM11181 |
PEG4-SPDP
PEG4-SPDP 是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联药物 (ADC)。 |
1305053-43-3 |
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KM4309 |
Phe-Lys(Fmoc)-PAB
Phe-Lys(Fmoc)-PAB 是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联药物 (ADC)。 |
2149584-03-0 | 98% |
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KM10823 |
Phe-Lys(Trt)-PAB
Phe-Lys(Trt)-PAB 是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联药物 (ADC)。 |
1116085-99-4 |
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KM11130 |
PPC-NB
PPC-NB 是一种谷胱甘肽可降解 (cleavable) 的 linker,用于抗体偶联药物 (ADC)。 |
1887040-81-4 |
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KM12992 |
PPC-NHS ester
PPC-NHS ester 是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联药物 (ADC)。 |
107348-47-0 |
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KM7025 |
Propargyl-C1-NHS ester
Propargyl-C1-NHS ester 是一种不可降解的 linker,可用于合成抗体偶联药物 (ADC) 。 |
132178-37-1 | 95% |
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KM11015 |
Propargyl-C2-NHS ester
Propargyl-C2-NHS ester 是一种不可降解的 linker,可用于合成抗体偶联药物 (ADC) 。 |
906564-59-8 |
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KM10103 |
Propargyl-O-C1-amido-PEG2-C2-NHS ester
Propargyl-O-C1-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) 。 |
2101206-30-6 |
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KM11391 |
Propargyl-O-C1-amido-PEG4-C2-NHS ester
Propargyl-O-C1-amido-PEG4-C2-NHS ester 是一种不可降解的含 4 个单元 PEG 的 linker,可用于合成抗体偶联药物 (ADC) 。 |
2101206-92-0 |
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KM6546 |
Propargyl-PEG2-acid
Propargyl-PEG2-acid 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)。Propargyl-PEG2-acid 还是一种 PROTAC linker,属于 PEG 类,可用于合成 PROTAC 分子。 |
1859379-85-3 | ≥98% |
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KM15148 |
Propargyl-PEG2-amine
Propargyl-PEG2-amine 是一种不可降解 (non-cleavable) 的 ADC linker,用于抗体偶联药物 (ADCs) 的合成。Propargyl-PEG2-amine 是一种 PROTAC linker,属于 PEG 类。Propargyl-PEG2-NH2 可用于合成一系列 PROTAC 分子。 |
944561-44-8 | ≥98% |
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KM10969 |
Propargyl-PEG4-Br
Propargyl-PEG4-Br 是一种 PROTAC 连接桥,属于 PEG 类。Propargyl-PEG4-Br 可用于合成一系列 PROTAC 分子。Propargyl-PEG4-Br 是一种不可降解 (non-cleavable) 的 ADC 连接桥,用于抗体药物结合物 (ADCs) 的合成。 |
1308299-09-3 |
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