1. Immunology/Inflammation
  2. CD20 CD3
  3. Glofitamab

Glofitamab  (Synonyms: 格菲妥单抗; RO7082859)

目录号: HY-P99024 纯度: ≥99.0%
COA

Glofitamab (RO7082859) 是一种与 T 细胞结合的双特异性抗体,具有新颖的 2:1 结构,即能够双价结合 B 细胞上的 CD20,并单价结合 T 细胞上的 CD3。Glofitamab 通过与恶性细胞上的 CD20 结合,激活 T 细胞,促进其增殖并杀死肿瘤细胞。Glofitamab 能够在复发或难治性的 B 细胞非霍奇金淋巴瘤 (B-NHL) 中诱导持久的完全缓解。

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CAS No. : 2229047-91-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Glofitamab (RO7082859) is a T-cell-engaging bispecific antibody possessing a novel 2:1 structure with bivalency for CD20 on B cells and monovalency for CD3 on T cells. Glofitamab leads to T-cell activation, proliferation, and tumor cell killing upon binding to CD20 on malignant cells. Glofitamab induces durable complete remissions in relapsed or refractory B-Cell non-Hodgkin lymphoma (B-NHL)[1][2][3][4].

同型

Human IgG1 kappa

推荐同型对照抗体
种属

Humanized

体外研究
(In Vitro)

Glofitamab (0.1 µg/mL, 48 小时) 与 FAP-IL2v (HY-P99902) 或 FAP-4-1BBL 联合使用刺激淋巴瘤肿瘤微环境 (TMEs) 中 CD8+ 肿瘤浸润淋巴细胞 (TILs) 上 4- 1bb (CD137) 的表达和增强型弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞死亡[4]
Glofitamab (0.2-200 ng/mL, 16 小时) 介导的 DLBCL 细胞杀伤作用需要形成稳定的 T 效应细胞-肿瘤细胞突触[5]
Glofitamab 对经 Obinutuzumab (Gpt) (HY-P9910) 预处理瞬时降低的 T 淋巴细胞亚群,NK 细胞和单核细胞无影响[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Glofitamab (0.3-100 μg/kg,单剂量静脉注射) 可诱导食蟹猴体内细胞因子 (IL-1Ra, IL-2, IL-5, IL-6, IL-8, IL-10, G-CSF, IFN-γ 和 TNF-α) 水平呈剂量依赖性升高[3]
Glofitamab (0.5 mg/kg, 静脉注射, 单剂量) 在小鼠中诱导早期和持久的 T 细胞结合和活性[5]

Glofitamab (静脉注射, 单次剂量) 在有或没有 Obinutuzumab (Gpt: 50 mg/kg) 处理的猕猴中的药代动力学参数 (MeSt: 机制研究;MTD: 最大耐受剂量)[3]

Study Gpt Dose (μg/kg) CL(mL/day/kg) Vc(mL/kg) T1/2 (days) Cmax (μg/mL) AUClast/dose(h·μg/mL/μg/kg)
MTD No 0.3 nd nd nd 0.00374/0.00663 nd
MTD No 1 nd 45.6/nd nd 0.0188/nd 0.0162/nd
MTD No 3 864/920 35.8/31.9 0.218/0.180 0.0704/0.0798 0.0218/0.0234
MTD No 10 735/656 26.7/24.6 0.143/0.159 0.318/0.354 0.0290/0.0339
MTD No 30 600/653 27.9/36.1 0.173/0.151 0.958/0.759 0.0397/0.0335
MTD No 100 190/290 34.9/41.6 0.203/0.113 2.74/2.29 0.126/0.0826
MeSt No 100 384±106 43.2±7.26 0.314±0.158 2.22±0.384 0.0679±0.0246
MeSt Yes 100 81.7±18.3 41.1±5.59 2.82±0.959 2.56±0.320 0.308±0.0773

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cynomolgus Monkeys[3]
Dosage: 0.3-100 μg/kg
Administration: i.v., a single dose, collected samples for cytokine measurements predose, 4, 24, 96 and 168 h post-dosing
Result: Resulted in cytokine levels peaked at 4 h post dose, with levels returning to baseline after 96 h for most cytokines in Cynomolgus Monkeys.
Animal Model: NSG mice co-injected with WSU and DLCL2 tumor cells and HSC-NSG-derived T cells[5]
Dosage: 0.5 mg/kg
Administration: i.v., a single dose, imaged 24, 48 or 72 hours post treatment
Result: Resulted in a higher frequency and longer duration of T cell-tumor cell interactions in mice, not only at early, but also at late time points.
Clinical Trial
CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

格菲妥单抗

运输条件

Shipping with dry ice.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

Format
  • IgG1-kappa/lambda with domain crossover, trivalent
Biological Activity
  • Flow cytometry analysis of Jurkat cells labelling CD3 with Glofitamab at 200 nM (Red). Goat anti human IgG Fc (Alexa Fluor488) was used as the secondary antibody at 1/1000 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Gray).
  • Flow cytometry analysis of Raji cells labelling CD20 with Glofitamab at 20 nM (Red). Goat anti human IgG Fc (Alexa Fluor488) was used as the secondary antibody at 1/1000 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Gray).
纯度 & 产品资料

纯度: 99.80%

参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Glofitamab
目录号:
HY-P99024
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