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VCMMAE (mc-vc-PAB-MMAE) 是一种用于 ADC 的药物-接头偶联物,具有抗癌活性,它由 MMAE 和 Vc 连接而成。
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VCMMAE (mc-vc-PAB-MMAE) 是一种用于 ADC 的药物-接头偶联物,具有抗癌活性,它由 MMAE 和 Vc 连接而成。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 245 | 现货 | |
5 mg | ¥ 383 | 现货 | |
10 mg | ¥ 549 | 现货 | |
25 mg | ¥ 987 | 现货 | |
50 mg | ¥ 1,620 | 现货 | |
100 mg | ¥ 2,390 | 现货 |
产品描述 | VCMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity. |
体外活性 | MMAE通过计划和剂量依赖的方式使结直肠癌和胰腺癌细胞对IR敏感,其机制与有丝分裂阻滞相关。Monomethyl auristatin E (MMAE) 在CD30+癌细胞内从SGN-35中高效释放,并由于其膜透性,具备对旁观者细胞施加细胞毒活性的能力。辐射增敏作用通过减少辐照细胞的克隆存活率和增加DNA双链断裂得以证实。 |
体内活性 | Monomethyl auristatin E (MMAE) 与 IR 结合使用,能增强 DNA 损伤信号传导和 CHK1 激活,从而延缓肿瘤生长。针对肿瘤的 ACPP-cRGD-MMAE 与 IR 共同作用,在异种移植模型中产生了更为显著且持久的肿瘤退缩效果。 |
细胞实验 | Monomethyl auristatin E is reconstituted in DMSO at a concentration of 5 nM. Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. 30 μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. |
动物实验 | 6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system. |
别名 | mc-vc-PAB-MMAE |
分子量 | 1316.63 |
分子式 | C68H105N11O15 |
CAS No. | 646502-53-6 |
Smiles | CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)C=CC2=O)C(C)C)cc1)C(C)C |
密度 | 1.196 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: 54 mg/mL |
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