Drug-Linker Conjugates
rug-linker complexes consist of two parts: a highly toxic drug which is a small molecule that interacts with intracellular targets and functions as agents to block or disrupt crucial cellular metabolic pathways and eventually lead to cell death, and a linker which facilitates the conjugation of ADC toxins to antibodies and in the meantime, dictates the release mechanism of an ADC. Pre-assembled drug-linker complexes can conjugate to ready-to-go antibody to speed up new antibody-drug conjugate (ADC) development processes.The Drug-Linker Conjugates can expand the utility of mAbs and improve their potency and effectiveness; the antibodies are thus used as a means to target and delivery a toxic payload to the selected diseased tissue.
The site-specific conjugations of Drug-Linker to an antibody may involve genetic engineering of the mAb to introduce discrete, available cysteines or non-natural amino acids with an orthogonally-reactive functional group handle such as an aldehyde, ketone, azido, or alkynyl tag. These site-specific approaches not only increase the homogeneity of ADCs but also enable novel bio-orthogonal chemistries that utilize reactive moieties other than thiol or amine. The cytotoxic drug, monomethyl auristatin E (MMAE), is conjugated to the three trastuzumab variants using a protease cleavable linker and shows in vivo therapeutic efficacy.
The site-specific conjugations of Drug-Linker to an antibody may involve genetic engineering of the mAb to introduce discrete, available cysteines or non-natural amino acids with an orthogonally-reactive functional group handle such as an aldehyde, ketone, azido, or alkynyl tag. These site-specific approaches not only increase the homogeneity of ADCs but also enable novel bio-orthogonal chemistries that utilize reactive moieties other than thiol or amine. The cytotoxic drug, monomethyl auristatin E (MMAE), is conjugated to the three trastuzumab variants using a protease cleavable linker and shows in vivo therapeutic efficacy.
Antibody Drug Conjugates (ADC)
Drug-Linker Conjugates
-
Mc-VC-PAB-SN38
产品货号 : M35101
cas no: 1801838-28-7
Mc-VC-PAB-SN38 由可降解 (cleavable) 的 ADC linker (Mc-VC-PAB) 和 SN38 组成,SN38 是一种 DNA 拓扑异构酶 I 抑制剂。Mc-VC-PAB-SN38 可用于合成抗体偶联活性分子 (ADC)。 -
Vc-MMAD
产品货号 : M33562
cas no: 1401963-17-4
Vc-MMAD 由 linker (Val-Cit) 和微管抑制剂 MMAD 组成。Vc-MMAD 可用于偶联抗体。 -
CL2A-SN-38
产品货号 : M21771
cas no: 1279680-68-0
CL2A-SN-38 是一种药物-接头缀合物,由有效的 DNA 拓扑异构酶 I 抑制剂 SN-38 和接头 CL2A 组成,用于制备抗体药物缀合物 (ADC)。 -
SuO-Val-Cit-PAB-MMAE
产品货号 : M16945
cas no: ——
抗体-药物缀合物的药物-接头缀合物,使用抗有丝分裂剂单甲基阿里他汀 E (MMAE),通过可裂解肽 SuO-Val-Cit-PAB 连接。 -
MAL-di-EG-Val-Cit-PAB-MMAE
产品货号 : M16944
cas no: ——
抗体-药物缀合物的药物-接头缀合物,使用抗有丝分裂剂单甲基阿里他汀 E (MMAE),通过可裂解肽 SuO-Val-Cit-PAB 连接。