中文名 | 单甲基奥瑞他汀E |
英文名 | VcMMAE |
别名 | 单甲基奥瑞他汀E 化合物VCMMAE VCMMAE游离态 VCMMAE 单甲基奥瑞他汀E 马来酰亚胺己酰基-缬氨酸-瓜氨酸-对氨基苄氧羰基单甲基耳他汀 E 马来酰亚胺己酰基-缬氨酸-瓜氨酸-对氨基苄氧羰基单甲基奥瑞他汀 E |
英文别名 | VeMMAE VcMMAE MC-VC-PAB-MMAE MC-Val-Cit-PAB-MMAE MC-VC-PAB-MMAE VCMMAE BRENTUXIMAB IMPURITY 2 (VEDOTIN) maleimido-caproyl-val-Cit-PAB-MMAE MC-VC-PAB-MMAE,MC-Val-Cit-PAB-MMAE Maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl-monomethyl auristatin E 4-((S)-2-((S)-2-(6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)-5-ureidopentanamido)benzyl((S)-1-(((S)-1-(((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-y |
CAS | 646502-53-6 |
化学式 | C68H105N11O15 |
分子量 | 1316.63 |
密度 | 1.196±0.06 g/cm3(Predicted) |
沸点 | 1347.6±65.0 °C(Predicted) |
溶解度 | DMSO: ≥ 54 mg/mL |
酸度系数 | 13.29±0.70(Predicted) |
存储条件 | Sealed in dry,Room Temperature |
物化性质 | 生物活性 VcMMAE (mc-vc-PAB-MMAE),一种具有缬氨酸-瓜氨酸(Vc)接头的MMAE衍生物,是具有抗肿瘤活性的antibody-drug conjugate (ADC)。MMAE是一种合成的抗肿瘤药,在体外可以有效地从VcMMAE释放出来并发挥细胞毒活性。 |
体外研究 | Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30 + cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells. MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells. |
体内研究 | Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.76 ml | 3.798 ml | 7.595 ml |
5 mM | 0.152 ml | 0.76 ml | 1.519 ml |
10 mM | 0.076 ml | 0.38 ml | 0.76 ml |
5 mM | 0.015 ml | 0.076 ml | 0.152 ml |
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