CAS: 159857-81-5; 4-((S)-2-((S)-2-(6-(2,5-Dioxo-2,5-Dihydro-1H-Pyrrol-1-yl)Hexanamido)-3-Methylbutanamido)-5-Ureidopentanamido)Benzyl (4-Nitrophenyl) Carbonate

上下游产品

N-[6-(2,5-二氢-2,5-二氧代-1H-吡咯-1-基)-1-氧代己基]-L-缬氨酰-N5-(氨基甲酰基)-N-[4-(羟甲基)苯基]-L-鸟氨酰胺 6-(2,5-Dioxo-2,5-Dihydro-1H-Pyrrol-1-yl)-N-((S)-1-(((S)-1-((4-(Hydroxymethyl)Phenyl)Amino)-1-Oxo-5-Ureidopentan-2-yl)Amino)-3-Methyl-1-Oxobutan-2-yl)Hexanamide 159857-80-4
[(S)-1-[[(S)-1-[[4-(羟甲基)苯基]氨基]-1-氧代-5-脲基戊烷-2-基]氨基]-3-甲基-1-氧代丁-2-基]氨基甲酸(9H-芴-9-基)甲酯 (9H-Fluoren-9-yl)Methyl ((S)-1-(((S)-1-((4-(Hydroxymethyl)Phenyl)Amino)-1-Oxo-5-Ureidopentan-2-yl)Amino)-3-Methyl-1-Oxobutan-2-yl)Carbamate 159858-22-7
Mc-Val-Cit-Oh

📜6-(马来酰亚胺基)己酸琥珀酰亚胺酯置于n,N-二异丙基乙胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 5.0H,反应生成马来酰亚胺基己酰-L-缬氨酸-L-瓜氨酸对氨基苄醇 对硝基苯基碳酸脂
参考文献:开发具有细胞毒性和免疫刺激的双功能抗 Pd-L1 抗体 Mmae 偶联物
标题:开发具有细胞毒性和免疫刺激的双功能抗 Pd-L1 抗体 Mmae 偶联物
摘要:近年来,肿瘤免疫治疗,尤其是pd1/pd-L1抑制剂与化疗的联合治疗发展迅速.然而,化疗引起的全身副作用仍然是一个需要解决的关键问题.抗体药物偶联物 (Adc) 是一种特殊的靶标特异性前药,可大大改善化疗药物的治疗窗口.因此,设计 Pd-L1 靶向 Adc 是一个有趣的研究项目.在本研究中,我们首次证实商用抗pd-L1抗体atezolizumab比avelumab具有更好的内吞效率,更适合adc设计.然后,最流行的细胞毒性有效载荷 Mmae 通过经典二肽(缬氨酸-丙氨酸)接头与 Atezolizumab 偶联,以生成双功能 Pd-L1 Adc(adc 3).的体外细胞毒性试验表明adc的有效的肿瘤细胞抑制活性3,用ec 50个9.75纳米的值,以11.94纳摩.此外,体外pbmc 的共培养证明 Adc 3保留了 Atezolizumab 抗体的免疫激活作用.此外,Adc 3在人源化免疫系统
Doi:10.1016/j.Bioorg.2021.105366

专利信息

专利号:US-2025018051-A1
优先权日:2021-11-10
标题:Anthracycline derivative linker reagents, antibody-drug conjugates and methods
发明人：SALSA MATTEO; GASPARRI FABIO; ORSINI PAOLO; VALSASINA BARBARA
权利人:NERVIANO MEDICAL SCIENCES SRL
摘要:The present invention provides anthracycline-linker reagents for the preparation of therapeutic antibody-drug conjugate (ADC) compounds. n The present invention also provides therapeutic antibody-drug conjugate (ADC) compounds comprising anthracycline drug moieties, with biological activity against cancer cells. The compounds may inhibit tumor growth in mammals and may be useful for treating human cancer patients. n Aspects of the invention include methods of making, methods of preparing, methods of synthesis, methods of conjugation, and methods of purification of the anthracycline-linker reagents and of the antibody-drug conjugate compounds.

专利号:CN-115368435-B
优先权日:2022-09-06
标题 :Synthesis method of antibody-coupled drug linker SET0568

专利号:CN-119684399-A
优先权日:2024-12-23
标题 :Synthesis method of Val-Cit dipeptide linker