CL2A-SN-38是drug-linkerconjugate,由linkerCL2A和毒性分子SN-38连接而成的,可用来制备抗体偶联药物。CL2A-SN-38针对人类实体瘤表现出特异性的抗肿瘤作用。SN-38是一种DNATopoisomeraseI抑制剂。CL2A是一种不可降解(non-cleavable)的含PEG8-和三偶氮的PBC-肽-mclinker。CL2A通过pH敏感性降解,产生旁观者效应,并通过二硫键与抗体结合在半胱氨酸残基上。
Cas No. | 1279680-68-0 |
Canonical SMILES | O=C(O[C@](C1=C(CO2)C(N3CC4=C(CC)C5=CC(O)=CC=C5N=C4C3=C1)=O)(CC)C2=O)OCC6=CC=C(NC([C@H](CCCCN)NC(COCC(NCCOCCOCCOCCOCCOCCOCCOCCOCCN7N=NC(CNC(C8CCC(CN9C(C=CC9=O)=O)CC8)=O)=C7)=O)=O)=O)C=C6 |
分子式 | C73H97N11O22 |
分子量 | 1480.61 |
溶解度 | DMSO: 100 mg/mL (67.54 mM) |
储存条件 | -20℃, stored under nitrogen, away from moisture |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond[1]. [1]. Cardillo TM, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69. |