VcMMAE
(Synonyms: 单甲基奥瑞他汀E,MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE) 目录号 : GC37891
A drug-linker molecule
Cas No.:646502-53-6
Sample solution is provided at 25 µL, 10mM.
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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)
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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. |
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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. |
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References: [1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897. |
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| Cas No. | 646502-53-6 | SDF | |
| 别名 | 单甲基奥瑞他汀E,MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE | ||
| Canonical SMILES | CC(C)[C@@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(COC(N(C)[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N([C@@H]([C@@H](C)CC)[C@H](OC)CC(N2[C@@]([C@H](OC)[C@@H](C)C(N[C@H](C)[C@@H](O)C3=CC=CC=C3)=O)([H])CCC2)=O)C)=O)=O)=O)C=C1)=O)=O)NC(CCCCCN4C(C=CC4=O)=O)=O | ||
| 分子式 | C68H105N11O15 | 分子量 | 1316.63 |
| 溶解度 | DMSO: ≥ 54 mg/mL (41.01 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.7595 mL | 3.7976 mL | 7.5951 mL |
| 5 mM | 0.1519 mL | 0.7595 mL | 1.519 mL |
| 10 mM | 0.076 mL | 0.3798 mL | 0.7595 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet