863971-19-1
中文名称
MC-MMAF
英文名称
SGD 1269
CAS
863971-19-1
分子式
C49H76N6O11
分子量
925.161
MOL 文件
863971-19-1.mol
更新日期
2024/07/23 11:15:51
863971-19-1 结构式
基本信息
中文别名
化合物MCMMAFN-[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
英文别名
McMMAFMc-MMAF
SGD 1269
Mafodotin
SGD-1269(MCMMAF)
MaleiMidocaproyl MonoMethylauristatin F
N-[6-(2,5-Dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-N-methyl-L-valyl-L-valyl-(3R,4S,5S)-3-methoxy-5-methyl-4-(methylamino)heptanoyl-(αR,βR,2S)-β-methoxy-α-methyl-2-pyrrolidinepropanoyl-L-phenylalanine
L-Phenylalanine, N-[6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl]-N-methyl-L-valyl-L-valyl-(3R,4S,5S)-3-methoxy-5-methyl-4-(methylamino)heptanoyl-(αR,βR,2S)-β-methoxy-α-methyl-2-pyrrolidinepropanoyl-
(2S)-2-[[(2R,3R)-3-[(2S)-1-[(3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-[6-(2,5-dioxopyrrol-1-yl)hexanoyl-methylamino]-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl]-3-methoxy-2-methylpropanoyl]amino]-3-phenylpropan
所属类别
生物：蛋白与多肽物理化学性质
沸点1052.0±65.0 °C(Predicted)
密度1.167±0.06 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
溶解度DMSO : ≥ 100 mg/mL (108.09 mM)
酸度系数(pKa)3.56±0.10(Predicted)
形态Solid
颜色White to off-white
常见问题列表
drug-linke偶联化合物
Drug-Linker Conjugates可以扩展单克隆抗体的效用并提高其效力和有效性;因此，抗体用作将有毒有效负载靶向并递送至所选患病组织的手段。Drug-Linker与抗体的位点特异性结合可能涉及mAb的基因工程，以引入离散的，可用的半胱氨酸或非天然氨基酸与正交反应性官能团处理，如醛，酮，叠氮基或炔基标签。这些位点特异性方法不仅增加了ADC的均一性，而且还能够利用除硫醇或胺之外的反应性部分的新型生物正交化学。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。
生物活性
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)。靶点
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Auristatin
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体外研究
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.