646502-53-6
646502-53-6 結(jié)構(gòu)式
基本信息
VCMMAE游離態(tài)
MC-VC-PAB-MMAE VCMMAE
馬來酰亞胺己酰基-纈氨酸-瓜氨酸-對(duì)氨基芐氧羰基單甲基耳他汀 E
BRENTUXIMAB IMPURITY 2 (VEDOTIN)
馬來酰亞胺己?；?纈氨酸-瓜氨酸-對(duì)氨基芐氧羰基單甲基奧瑞他汀 E
VCMMAE/VCMMAE/MC-VC-PAB-MMAE/98%含量
VeMMAE
EOS-60990
MC-VC-PAB-MMAE
VC-MMAE
VC MMAE
MC-Val-Cit-PAB-MMAE
MC-VAL-CIT-PABC-MMAE
Brentuximab Impurity 1 (Vedotin)
maleimido-caproyl-val-Cit-PAB-MMAE
MC-VC-PAB-MMAE,MC-Val-Cit-PAB-MMAE
物理化學(xué)性質(zhì)
常見問題列表
VcMMAE (mc-vc-PAB-MMAE) 是一種生化試劑，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 (一種 tubulin 抑制劑) 和 Vc 連接而成。
VcMMAE（mc-vc-PAB-MMAE）是ADC的藥物連接物偶聯(lián)物，通過使用抗核分裂劑單甲基auristatin E（MMAE，微管蛋白抑制劑），通過溶酶體可裂解的二肽，纈氨酸- 瓜氨酸（vc）。
單甲基耳他汀E（MMAE）可從CD30 +癌細(xì)胞內(nèi)的SGN-35有效釋放，并且由于其膜通透性，能夠?qū)ε杂^者細(xì)胞發(fā)揮細(xì)胞毒活性。 MMAE以與有絲分裂阻滯相關(guān)的時(shí)間表和劑量依賴性方式使大腸和胰腺癌細(xì)胞對(duì)IR敏感。 放療后克隆形成存活率降低和DNA雙鏈斷裂增加證明了放射增敏。
單甲基澳瑞他汀E（MMAE）與IR結(jié)合會(huì)導(dǎo)致腫瘤生長(zhǎng)延遲，在異種移植模型中，以IR靶向腫瘤的ACPP-cRGD-MMAE會(huì)產(chǎn)生更穩(wěn)定且顯著延長(zhǎng)的腫瘤消退。
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Auristatin
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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.
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.