Atezolizumab

目录号:A2004 别名: MPDL3280A 适用于非人源化小鼠

For research use only. Not for use in humans.

Atezolizumab是人源、IgG1单克隆抗体,阻止PD-L1与PD-1和B7.1的相互作用,但不影响PD-L2与PD-1的相互作用;MW:145 KD。

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RMB 5791.09 现货
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质量管理及产品安全说明书

PD-1/PD-L1抑制剂选择性比较

生物活性

产品描述 Atezolizumab是人源、IgG1单克隆抗体,阻止PD-L1与PD-1和B7.1的相互作用,但不影响PD-L2与PD-1的相互作用;MW:145 KD。
靶点
hPD-L1 [2]
(Cell-free assay)
0.4 nM(Kd)
体外研究

Atezolizumab的主要特征是,它是一种FcγR结合缺陷的抗体抑制剂,它不能与吞噬细胞上的Fc受体结合,因而不会引起抗体依赖性的细胞毒性(ADCC)。Atezolizumab的处理会引起细胞因子的改变,包括IL-18, IFNγ, CXCL11的瞬时增加和IL-6的瞬时减少。处于增殖状态的CD8+ T细胞数目在atezolizumab处理后会增多。

体内研究 Atezolizumab通过阻止PD-L1/PD-1免疫检查点,减少肿瘤微环境中的免疫抑制信号,同时增强T细胞介导的对抗肿瘤的免疫反应。最开始对Atezolizumab的药代动力学的研究在cynomolgus monkeys和小鼠中进行,其分布容积约为血浆中体积。给药24小时后,atezolizumab在体内生物分布于脾脏、肾脏、肝脏、心脏和肌肉(按数量级排序)。在携瘤动物中,Atezolizumab也会在肿瘤中积累,最开始是在肿瘤的推挤边界(pushing order),进而向肿瘤核心区域进展,尤其是肿瘤坏死时。Atezolizumab的药代动力曲线是剂量依赖性的(非线性)。给药后24-48小时,当血浆浓度>0.5 μg/mL时,循环的CD4和CD8 T细胞中,PD-L1受体被atezolizumab占据饱和[1]。Atezolizumab与PD-L1的结合亲和力在猴子和人类中类似[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:
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  • Objective: Antibody-dependent cellular cytotoxicity (ADCC)
    Cells: UDHL cells(lymphoma cell line), 293 cells and human PBLs
    Concentrations: --
    Incubation Time: --
    Method: In an in vitro assay for antibody dependent cellular cytotoxicity (using human PBLs as effectors), the engineered antibody was unable to mediate the killing of two cell lines transfected with human PD-L1, while efficient killing was observed using the unmodified 'wild-type' antibody.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/25428504

    Objective: Determine the binding of [111In]PD-L1-mAb to tumor cell lines
    Cells: NCI-H2444(Lung Cancer cell line), MDAMB231(Breast Cancer cell line),etc
    Concentrations: 1 μCi/100μl
    Incubation Time: 1 h
    Method: Incubating 1 μCi of [111In]PD-L1-mAb with 1×106cells (in triplicate for each cell line) for 1h at 37°C. PD-L1 blocking was performed by adding a 10-fold molar equivalent excess of the non-labeled mAb. After incubation, cells were washed three times with cold PBS prior to counting on an automated gamma counter.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/26848870

    Atezolizumab can apply to humanized mice, non-humanized mice (eg: C57BL/6 mice), peripheral blood and other related assays (Only for Reference)
动物实验:
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  • Objective: To determine the effect of anti-hPD-L1 antibody on human PD-L1-expressing mouse tumor model
    Animal Models: Female C57BL/6 mice were subcutaneous inoculated with MC-38-hPD-L1 cells
    Formulation: PBS
    Dosages: 1 mg/kg, 3 mg/kg, 10 mg/kg
    Administration: i.p.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/?term=28202921

    Objective: Developed and evaluated radiolabeled [111In] PD-L1-mAb and near-infrared dye conjugated NIR-PD-L1-mAb (Atezolizumab) for non-invasive imaging of PD-L1 expression in tumors
    Animal Models: NSG mice (humanized mice) were implanted subcutaneously with CHO-PDL1, CHO, H2444 H1155 cells and orthotopically in the upper mammary fat pads with MDAMB231 and SUM149 cells
    Formulation: 14.8 MBq (400 μCi) of [111In]PD-L1-mAb or 22 μg of NIR-PD-L1-mAb
    Dosages: 200 μg per injection
    Administration: i.v.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/26848870

    Atezolizumab can apply to humanized mice, non-humanized mice (eg: C57BL/6 mice), peripheral blood and other related assays (Only for Reference)

抗体信息

Formulation PBS buffer, pH 7.2
Isotype Human IgG
Source CHO cells
Storage Store at -80°C and avoid freeze-thaw cycles.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID