ADCs Linker/Click Chemistry
An ADC consists of three key components: a drug or payload, a linker, and an antibody. There are two broad categories of ADC linkers, namely cleavable and non-cleavable linkers.The former can be divided into several sub-types including: Acid-labile linkers, Protease cleavable linkers, Disulfide linkers; In contrast, the non-cleavable linkers have higher blood stability and often rely on internalization kinetics, facile lysosomal delivery, and ensuing ADC degradation to yield cancer cell apoptosis. Non-cleavable linkers account for about 20 % of the ADCs in clinical testing. Clearly, there is inter-dependency between the linker and conjugation chemistry. The choice of linker-conjugation chemistry affects ADC’s stability, efficacy, pharmacokinetics, homogeneity, and biophysical integrity. There are several conjugation strategies: Conjugation through lysine amino acids, Conjugation via cysteine residues by reducing ‘inter-chain’ native disulfide bonds, Increasing the homogeneity of the ADC by sitespecific conjugation via genetically engineered amino acid alteration, Enzyme-mediated conjugation and incorporation of an unnatural amino acid.
References:
1.Bakhtiar R. Biotechnol Lett. 2016 Oct;38(10):1655-64.
References:
1.Bakhtiar R. Biotechnol Lett. 2016 Oct;38(10):1655-64.
Antibody Drug Conjugates (ADC)
ADCs Linker/Click Chemistry
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Bz-(Me)Tz-NHS
产品货号 : M37353
cas no: 1454558-58-7
Bz-(Me)Tz-NHS 是一种含有甲基四嗪基团的点击化学试剂。Bz-(Me)Tz-NHS 是用于无铜点击共轭的第三代 Click-Linker。 -
Mal-amide-PEG8-Val-Ala-PAB-PNP
产品货号 : M37128
cas no: 2210247-59-7
Mal-amide-PEG8-Val-Ala-PAB-PNP 是一种可降解 (cleavable) 的 ADC linker,用于合成可用于合成抗体偶联活性分子 (ADC)。 -
6-Azido-hexylamine
产品货号 : M35207
cas no: 349553-73-7
6-Azido-hexylamine是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联活性分子 (ADC)。6-Azido-hexylamine 是一种点击化学试剂。它含有 Azide 基团,可以和含有 Alkyne 基团的分子发生铜催化的叠氮-炔环加成反应(CuAAc)。还可以和含有 DBCO 或 BCN 基团的分子发生菌株促进的炔-叠氮环加成反应 (SPAAC)。 -
SPP
产品货号 : M33560
cas no: 341498-08-6
SPP 是一种可降解的含二硫键的 linker,可用于形成细胞毒性化合物-linker 偶联物。 -
SPDMV
产品货号 : M33559
cas no: 890409-85-5
SPDMV 是一种可降解 (cleavable) 的 ADC linker,可用于合成抗体偶联活性分子 (ADC)。