Avelumab (Anti-Human PD-L1, Human Antibody)
(Synonyms: 阿维鲁单抗; Anti-Human PD-L1, Human Antibody; MSB 0010718C; MSB0010718C) 目录号 : GC31719
Avelumab (Anti-Human PD-L1, Human Antibody)是一种静脉给药的完全人源化IgG1单克隆抗体。
Cas No.:1537032-82-8
Sample solution is provided at 25 µL, 10mM.
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Avelumab (Anti-Human PD-L1, Human Antibody) is an intravenously (i.v.) administered fully human IgG1 monoclonal antibody (mAb)[1]. Avelumab can inhibit the interaction between PD-L1 and PD-1 and mediate antibody-dependent cell-mediated cytotoxicity (ADCC) through retention of its native FcR, leading to the reinvigoration of effector T cells [2]. Avelumab has been widely used to inhibit tumor progression in different tumor models and to develop novel combination therapies to enhance synergistic anti-tumor effects[3].
In vitro, Avelumab treatment at 20μg/ml for 7 days increased IFN-γ levels and decreased IL-5 concentrations in peripheral blood mononuclear cells (PBMC)[4]. Incubation with 2μg/ml Avelumab for 30min increased the sensitivity of IFN-γ-treated UM-Chor1 cells to natural killer (NK) lysis[5]. Treatment with Avelumab at 2μg/ml for 24h promoted NK cell disinhibition and enhanced the cytotoxicity against HPV-positive cervical cancer cells[6].
In vivo, Avelumab treatment, at a dose of 400µg/100µl intraperitoneally every three days for 9 days, significantly inhibited tumor growth in C57BL/6 mice bearing MB49 subcutaneous tumors and substantially improved 60-day survival[7]. Intraperitoneal injection of Avelumab at a dose of 400µg every 2 days for one week significantly delayed MC38 tumor growth in C57BL/6 mice and increased CD8+ T cell frequency in mouse spleen[8].
References:
[1] Kim E S. Avelumab: first global approval[J]. Drugs, 2017, 77(8): 929-937.
[2] Collins J M, Gulley J L. Product review: avelumab, an anti-PD-L1 antibody[J]. Human vaccines & immunotherapeutics, 2019, 15(4): 891-908.
[3] Bourhis J, Stein A, de Boer J P, et al. Avelumab and cetuximab as a therapeutic combination: An overview of scientific rationale and current clinical trials in cancer[J]. Cancer treatment reviews, 2021, 97: 102172.
[4] Grenga I, Donahue R N, Lepone L M, et al. A fully human IgG1 anti‐PD‐L1 MAb in an in vitro assay enhances antigen‐specific T‐cell responses[J]. Clinical & translational immunology, 2016, 5(5): e83.
[5] Fujii R, Friedman E R, Richards J, et al. Enhanced killing of chordoma cells by antibody-dependent cell-mediated cytotoxicity employing the novel anti-PD-L1 antibody avelumab[J]. Oncotarget, 2016, 7(23): 33498.
[6] Liu H, Zhou S, Liu J, et al. Lirilumab and avelumab enhance anti-HPV+ cervical cancer activity of natural killer cells via Vav1-dependent NF-κB disinhibition[J]. Frontiers in oncology, 2022, 12: 747482.
[7] Vandeveer A J, Fallon J K, Tighe R, et al. Systemic immunotherapy of non-muscle invasive mouse bladder cancer with avelumab, an anti–PD-L1 immune checkpoint inhibitor[J]. Cancer immunology research, 2016, 4(5): 452-462.
[8] Fallon J K, Vandeveer A J, Schlom J, et al. Enhanced antitumor effects by combining an IL-12/anti-DNA fusion protein with avelumab, an anti-PD-L1 antibody[J]. Oncotarget, 2017, 8(13): 20558.
Avelumab (Anti-Human PD-L1, Human Antibody)是一种静脉给药的完全人源化IgG1单克隆抗体[1]。Avelumab能抑制PD-L1与PD-1之间的相互作用，并通过保留天然的FcR介导抗体依赖性细胞介导的细胞毒性（ADCC），从而重新激活效应T细胞[2]。Avelumab已被广泛用于抑制不同肿瘤模型中的肿瘤进展，并开发新型联合疗法以增强协同抗肿瘤效应[3]。
在体外，使用20µg/ml的Avelumab处理7天，提高了外周血单个核细胞（PBMC）中IFN-γ的水平并降低了IL-5的浓度[4]。用2µg/ml的Avelumab孵育30分钟，增加了经IFN-γ处理的UM-Chor1细胞对自然杀伤（NK）细胞裂解的敏感性[5]。使用2µg/ml的Avelumab处理24小时，促进了NK细胞的抑制解除，并增强了NK细胞对HPV阳性宫颈癌细胞的细胞毒性[6]。
在体内，每隔三天腹腔注射Avelumab（剂量为400µg/100µl），持续9天，显著抑制了携带MB49皮下肿瘤的C57BL/6小鼠中的肿瘤生长，并大幅提高了60天存活率[7]。每隔两天腹腔注射Avelumab（剂量为400µg），持续一周，显著延迟了C57BL/6小鼠中MC38肿瘤的生长，并增加了小鼠脾脏中CD8+ T细胞的频率[8]。
| Cell experiment [1]: | |
Cell lines | UM-Chor1 cells |
Preparation Method | UM-Chor1 cells were treated with 50ng/ml IFN-γ for 24 hours. Cells were then seeded in 6-well round-bottom culture plates at a density of 5×104 cells/well and incubated with 2μg/ml Avelumab for 30min at room temperature. Subsequently, 2.5×107 NK cells/well were added with a 50:1 ratio of effector cells to target cells. Four hours later, tumor cells were harvested and stained with antibodies for flow cytometry analysis. |
Reaction Conditions | 2μg/ml; 30min |
Applications | Avelumab treatment increased UM-Chor1 cells' sensitivity to NK-cell lysis. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Tumor injection was performed by subcutaneous injection of 1×105 MB49 parental cells into the right shaved abdomen of C57BL/6 mice. Tumor growth was measured with a vernier caliper, and mice were randomly assigned to treatment groups 8 days after inoculation. Treatment began on day 9 with an intraperitoneal injection of 400µg/100µl of Avelumab every three days for nine days. Tumors were measured twice a week throughout the study, and tumor volume was calculated according to the following formula: volume=(width)2×(length)/2. |
Dosage form | 400µg/100µl; every three days for nine days; i.p. |
Applications | Avelumab treatment significantly suppressed tumor growth in C57BL/6 mice bearing MB49 subcutaneous tumors and substantially improved mouse survival. |
References: | |
| Cas No. | 1537032-82-8 | SDF | |
| 别名 | 阿维鲁单抗; Anti-Human PD-L1, Human Antibody; MSB 0010718C; MSB0010718C | ||
| Canonical SMILES | [Avelumab] | ||
| 分子式 | 分子量 | 143.8 kDa | |
| 溶解度 | Soluble in DMSO | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 7 μL | 34.8 μL | 69.5 μL |
| 5 mM | 1.4 μL | 7 μL | 13.9 μL |
| 10 mM | 0.7 μL | 3.5 μL | 7 μL |
| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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.
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