VcMMAE

A drug-linker molecule

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库存: 现货

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促销价

数量
5mg

￥425.00

340.00

- +
10mg

￥600.00

480.00

- +
50mg

￥1687.00

1350.00

- +
100mg

￥2537.00

2030.00

- +
500mg

￥4700.00

3760.00

- +

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货号: ajce60024
CAS: 646502-53-6
别名: 单甲基奥瑞他汀E,MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE
分子式: C68H105N11O15
分子量: 1316.63
纯度: >98%
溶解度: DMSO: ≥ 54 mg/mL (41.01 mM)
储存: Store at -20°C
库存: 现货

Background

VcMMAE is a drug-linker molecule that has been used in the synthesis of antibody-drug conjugates (ADCs).¹,² It contains a maleimidocaproyl (Mc) group that can be conjugated to an antibody, a protease-cleavable peptide linker, and the antimitotic and anticancer agent monomethyl auristatin E .

1.Chuprakov, S., Ogunkoya, A.O., Barfield, R.M., et al.Tandem-cleavage linkers improve the in vivo stability and tolerability of antibody-drug conjugatesBioconjug. Chem.32(4)746-754(2021) 2.Dimou, M., Papageorgiou, S.G.S., N., Katodritou, E., et al.Real-life experience with the combination of polatuzumab vedotin, rituximab, and bendamustine in aggressive B-cell lymphomasHematol. Oncol.39(3)336-348(2021)

Protocol

Cell experiment:

Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. 30μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. Blots are developed by ECL.

Animal experiment:

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.

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.