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VCMMAE

VCMMAE

产品编号 T4232   CAS 646502-53-6
别名: mc-vc-PAB-MMAE

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 Chemical Structure
VCMMAE, CAS 646502-53-6
规格 价格/CNY 货期 数量
5 mg ¥ 383 现货
10 mg ¥ 549 现货
25 mg ¥ 996 现货
50 mg ¥ 1,625 现货(一周内)
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: VCMMAE (T4232)
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纯度: 100%
纯度: 99.58%
纯度: 99.27%
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生物活性
化学信息
存储 & 溶解度
参考文献
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 sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, owing to its membrane permeability, it has the ability to exert cytotoxic activity on bystander cells. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells.
体内活性 Monomethyl auristatin E (MMAE) in combination with IR results in increased DNA damage signaling and activation of CHK1 that delay the tumor growth. Tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models.
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 54 mg/mL

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TargetMol Library Books参考文献

1. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinicalal 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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相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 NO PAINS 化合物库 细胞骨架化合物库 已知活性化合物库 经典已知活性库 抗癌化合物库

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Keywords

VCMMAE 646502-53-6 Cytoskeletal Signaling Microtubule Associated mc-vc-PAB-MMAE inhibit Drug-Linker Conjugates for ADC Inhibitor Microtubule/Tubulin inhibitor

 

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