MC-MMAF
中文名称 | MC-MMAF |
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中文同义词 | N-[6-(2,5-二氢-2,5-二氧代-1H-吡咯-1-基)-1-氧代己基]-N-甲基-L-缬氨酰-L-缬氨酰基-(3R,4S,5S )-3-甲氧基-5-甲基-4-(甲氨基)庚酰基-(ΑR,ΒR,2S)-Β-甲氧基-Α-甲基-2-吡咯烷丙酰基-L-苯丙氨酸;化合物MCMMAF;MC-MMAF游离态;N-[6-(2,5-二氢-2,5-二氧代-1H-吡咯-1-基)-1-氧代己基]-N-甲基-L-缬氨酰-L-缬氨酰基-(3R,4S,5S )-3-甲氧基-5-甲基-4-(甲氨基)庚酰基-(ΑR,ΒR,2S)-Β-甲氧基-Α-甲基-2-吡咯烷丙酰基-L-苯丙氨酸 |
英文名称 | MC-MMAF |
英文同义词 | Mafodotin;MaleiMidocaproyl MonoMethylauristatin F;McMMAF;Mc-MMAF;SGD 1269;(S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N-methylhexanamido)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic aci;(S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N-methylhexanamido)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid;SGD-1269(MCMMAF) |
CAS号 | 863971-19-1 |
分子式 | C49H76N6O11 |
分子量 | 925.16 |
EINECS号 | |
相关类别 | 抑制剂;多肽抑制剂;抗体偶联药物中间体;生物试剂;Amino Acids & Derivatives, Aromatics, Pharmaceuticals, Intermediates & Fine Chemicals;ADCs |
Mol文件 | 863971-19-1.mol |
结构式 |
MC-MMAF 性质
沸点 | 1052.0±65.0 °C(Predicted) |
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密度 | 1.167±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:≥100mg/mL(108.09mM) |
酸度系数(pKa) | 3.56±0.10(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
Mc-MMAF(CAS: 863971-19-1)是由高效微管抑制剂Monomethyl auristatin F (MMAF) 与保护基团maleimidocaproyl偶联而成。MMAF(一甲基澳瑞他汀F)为抗微管蛋白化合物,能通过阻断微管聚合抑制细胞分裂,较MMAE毒性低。
VcMMAE(cas:646502-53-6)是抗体药物复合体的一部分 (drug-linker conjugate for ADC),具有抗癌活性,它由MMAE和Vc连接而成。McMMAF 是由高效微管抑制剂 Monomethyl auristatin F (MMAF) 与保护基团 maleimidocaproyl 偶联而成。MMAF 为抗微管蛋白化合物,能通过阻断微管聚合抑制细胞分裂,较 MMAE 毒性低,可用于抗体偶联药物 (ADC)。
Auristatin
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MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-15578 | MC-MMAF McMMAF | 863971-19-1 | 1mg | 613元 |
2024/08/19 | HY-15578 | MC-MMAF McMMAF | 863971-19-1 | 5mg | 1350元 |