VcMMAE (Synonyms: MC-VC-PAB-MMAE, Vedotin) |
| カタログ番号GC37891 |
VcMMAE (mc-vc-PAB-MMAE) は、抗有糸分裂剤であるモノメチル オーリスタチン E (MMAE、チューブリン阻害剤) を使用して強力な抗腫瘍活性を有する ADC の薬物-リンカー結合体であり、リソソームで切断可能なジペプチドであるバリンを介して結合しています。シトルリン（vc）。
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Cas No.: 646502-53-6
Sample solution is provided at 25 µL, 10mM.
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VcMMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
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[1]. 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[2].
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[2].
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897. [2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87. [3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.
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