阿特珠单抗 - CAS:1380723-44-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	阿特珠单抗
英文名称:	Atezolizumab
别名:	阿特朱单抗;阿特珠单抗 Atezolizumab;Tecentriq
CAS No:	1380723-44-3
CAS No:	1380723-44-3

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A10976 阿特珠单抗 ≥95% (psaitong)

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阿特珠单抗
CAS No：1380723-44-3

包装规格：

1mg 5mg in glass bottle

产品描述：

基本信息

产品编号：	A10976
产品名称：	Atezolizumab
CAS:	1380723-44-3	储存条件	粉末	-20℃	四年

分子式：			溶于液体
分子量
化学名：

生物活性

产品描述	一种人源化单克隆抗体 IgG1，抵抗程序性死亡因子配体1 (PD-L1)，用于癌症研究。
靶点	hPD-L1 (Cell-free assay) 0.4nM(Kd)
体外研究	Atezolizumab (anti-PD-L1)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 (anti-PD-L1)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>0.5μg/mL时，循环的CD4和CD8 T细胞中，PD-L1受体被atezolizumab占据饱和。Atezolizumab与PD-L1的结合亲和力在猴子和人类中类似。

推荐实验方法(仅供参考)

细胞实验：

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.

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: 1μCi/100μl
Incubation Time: 1 h
Method: Incubating 1μCi 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.

动物实验:

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: 1mg/kg, 3mg/kg, 10mg/kg
Administration: i.p.

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: 14.8MBq (400μCi) of [111In]PD-L1-mAb or 22μg of NIR-PD-L1-mAb
Dosages: 200μg per injection
Administration: i.v.