863971-19-1
中文名稱
MC-MMAF
英文名稱
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
2024/12/24 22:16:39
863971-19-1 結(jié)構(gòu)式
基本信息
中文別名
化合物MCMMAFN-[6-(2,5-二氫-2,5-二氧代-1H-吡咯-1-基)-1-氧代己基]-N-甲基-L-纈氨酰-L-纈氨?；?(3R,4S,5S )-3-甲氧基-5-甲基-4-(甲氨基)庚?；?(ΑR,ΒR,2S)-Β-甲氧基-Α-甲基-2-吡咯烷丙?；?L-苯丙氨酸
英文別名
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
所屬類別
生物：蛋白與多肽物理化學(xué)性質(zhì)
沸點(diǎn)1052.0±65.0 °C(Predicted)
密度1.167±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMSO : ≥ 100 mg/mL (108.09 mM)
酸度系數(shù)(pKa)3.56±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
drug-linke偶聯(lián)化合物
Drug-Linker Conjugates可以擴(kuò)展單克隆抗體的效用并提高其效力和有效性;因此，抗體用作將有毒有效負(fù)載靶向并遞送至所選患病組織的手段。Drug-Linker與抗體的位點(diǎn)特異性結(jié)合可能涉及mAb的基因工程，以引入離散的，可用的半胱氨酸或非天然氨基酸與正交反應(yīng)性官能團(tuán)處理，如醛，酮，疊氮基或炔基標(biāo)簽。這些位點(diǎn)特異性方法不僅增加了ADC的均一性，而且還能夠利用除硫醇或胺之外的反應(yīng)性部分的新型生物正交化學(xué)。Mc-MMAF（CAS: 863971-19-1）是由高效微管抑制劑Monomethyl auristatin F (MMAF) 與保護(hù)基團(tuán)maleimidocaproyl偶聯(lián)而成。MMAF(一甲基澳瑞他汀F)為抗微管蛋白化合物，能通過阻斷微管聚合抑制細(xì)胞分裂，較MMAE毒性低。
VcMMAE(cas:646502-53-6)是抗體藥物復(fù)合體的一部分 (drug-linker conjugate for ADC)，具有抗癌活性，它由MMAE和Vc連接而成。
生物活性
McMMAF 是由高效微管抑制劑 Monomethyl auristatin F (MMAF) 與保護(hù)基團(tuán) maleimidocaproyl 偶聯(lián)而成。MMAF 為抗微管蛋白化合物，能通過阻斷微管聚合抑制細(xì)胞分裂，較 MMAE 毒性低，可用于抗體偶聯(lián)藥物 (ADC)。靶點(diǎn)
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Auristatin
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體外研究
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.