MC-GGFG-Exatecan (MC-GGFG-DX8951) 是一种抗体偶联药物 (drug-linker conjugate for ADC),由DNA拓扑异构酶 I 抑制剂 DX8951 和蛋白酶可降解 (cleavable) 的 MC-GGFG 连接而成。MC-GGFG-Exatecan 表现出抗肿瘤活性,可用于制备 DX8951 抗体结合物 (ADC)。
生物活性
MC-GGFG-Exatecan (MC-GGFG-DX8951) is a drug-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC).
性状
Solid
IC50 & Target[1][2]
Camptothecins
体外研究(In Vitro)
In MC-GGFG-Exatecan, GGFG is selectively cleaved by lysosomal enzymes (presumably cathepsins). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
In MC-GGFG-Exatecan, GGFG is known to release drugs into tumor tissue without releasing them into peripheral circulation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Nakada T, et al. Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1542-1545.
溶解度数据
In Vitro: DMSO : 50 mg/mL (52.80 mM; Need ultrasonic)配制储备液