ADC Cytotoxin
Payload selection is another critical factor that defines the success of an ADC. An ideal ADC payload is a highly potent small molecule with lack of specificity. Currently, there are two broad categories of payloads
for conjugation to a mAb. The first category is referred to as radionuclide antibody conjugates (RACs), where a radionuclide emitting radiation penetrates into the targeted cells of the solid tumor to induce a sufficient
lethal response with no or minimal damage to the surrounding healthy cells. The second and a major category for antibody payloads include high potency synthetic or natural product small molecules. ADC payloads approved or under development are for the most part cytotoxic agents with picomolar or sub-picomolar potencies.
References:
1.Bakhtiar R. Biotechnol Lett. 2016 Oct;38(10):1655-64.
for conjugation to a mAb. The first category is referred to as radionuclide antibody conjugates (RACs), where a radionuclide emitting radiation penetrates into the targeted cells of the solid tumor to induce a sufficient
lethal response with no or minimal damage to the surrounding healthy cells. The second and a major category for antibody payloads include high potency synthetic or natural product small molecules. ADC payloads approved or under development are for the most part cytotoxic agents with picomolar or sub-picomolar potencies.
References:
1.Bakhtiar R. Biotechnol Lett. 2016 Oct;38(10):1655-64.
Antibody Drug Conjugates (ADC)
ADC Cytotoxin
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(rac)-Exatecan Intermediate 1
产品货号 : M37604
cas no: 102978-40-5
(rac)-Exatecan Intermediate 1 是 Exatecan Intermediate 1 (HY-42487) 的异构体。Exatecan Intermediate 1 (compound 6) 是 Exatecan (HY-13631) 的中间体,这是一种喜树碱类抗癌剂。Exatecan 通过与 DNA 发生相互作用来干扰肿瘤细胞的增殖和分裂,从而抑制肿瘤的生长。Exatecan 主要用于卵巢癌、肺癌和乳腺癌等多种癌症的研究。 -
AXC-666
产品货号 : M37595
cas no: 313350-30-0
AXC-666 是一种免疫激动剂,是 Imiquimod(HY-B0180) 衍生物。AXC-666 可用于合成抗体药物偶联物 (ADC)。 -
FL118-14-Propanol
产品货号 : M37546
cas no: 2821768-98-1
FL118-14-Propanol 是 FL118 衍生物。FL118-14-Propanol 合成的ADC分子对小鼠具有良好的抗肿瘤作用。 -
Duostatin 5
产品货号 : M37127
cas no: 2124210-34-8
Duostatin 5 是一种基于海兔毒素设计的细胞毒素 (cytotoxin),在 ADC 中可作为有效细胞毒素,具有合成步骤少、操作简单、质量控制难度小、化学合成过程更稳定等优点。 -
(4-NH2)-Exatecan
产品货号 : M35185
cas no: 2495742-21-5
(4-NH2)-Exatecan 是一种拓扑异构酶 (topoisomerase) 抑制剂,是 Exatecan 的衍生物,可用于合成抗体偶联活性分子 (ADC) (US20200306243A1, compound A)。