产品描述: | VcMMAE (mc-vc-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc). |
靶点: |
Auristatin;MicrotubuleAssociated |
体外研究: |
VcMMAE (MMAE) 在 CD30+ 癌细胞内从 SGN-35 有效释放,并且由于其膜渗透性,能够对旁观者细胞发挥细胞毒活性。MMAE 以与有丝分裂停滞相关的时间表和剂量依赖性方式使结直肠癌细胞和胰腺癌细胞对 IR 敏感。放射增敏作用表现为受照射细胞中克隆形成存活率下降和 DNA 双链断裂增加 |
体内研究: |
VcMMAE (MMAE) 与 IR 结合导致肿瘤生长延迟,肿瘤靶向 ACPP-cRGD-MMAE 与 IR 在异种移植模型中产生更稳健和显著延长的肿瘤消退 |
参考文献: |
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. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
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 |
50 mM |
0.015 ml |
0.076 ml |
0.152 ml |
|
注意: |
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