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

Glofitamab  (Synonyms: 格菲妥單抗; RO7082859)

目錄號(hào): HY-P99024 純度: ≥99.0%
COA 技術(shù)支持

Glofitamab (RO7082859) 是一種與 T 細(xì)胞結(jié)合的雙特異性抗體，具有新穎的 2:1 結(jié)構(gòu)，即能夠雙價(jià)結(jié)合 B 細(xì)胞上的 CD20，并單價(jià)結(jié)合 T 細(xì)胞上的 CD3。Glofitamab 通過與惡性細(xì)胞上的 CD20 結(jié)合，激活 T 細(xì)胞，促進(jìn)其增殖并殺死腫瘤細(xì)胞。Glofitamab 能夠在復(fù)發(fā)或難治性的 B 細(xì)胞非霍奇金淋巴瘤 (B-NHL) 中誘導(dǎo)持久的完全緩解。

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CAS No. : 2229047-91-8

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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
推薦同型對(duì)照抗體
種屬

Humanized
體外研究
(In Vitro)

Glofitamab (0.1 μg/mL, 48 小時(shí)) 與 FAP-IL2v (HY-P99902) 或 FAP-4-1BBL 聯(lián)合使用刺激淋巴瘤腫瘤微環(huán)境 (TMEs) 中 CD8+ 腫瘤浸潤淋巴細(xì)胞 (TILs) 上 4- 1bb (CD137) 的表達(dá)和增強(qiáng)型彌漫性大 B 細(xì)胞淋巴瘤 (DLBCL) 細(xì)胞死亡[4]。
Glofitamab (0.2-200 ng/mL, 16 小時(shí)) 介導(dǎo)的 DLBCL 細(xì)胞殺傷作用需要形成穩(wěn)定的 T 效應(yīng)細(xì)胞-腫瘤細(xì)胞突觸[5]。
Glofitamab 對(duì)經(jīng) Obinutuzumab (Gpt) (HY-P9910) 預(yù)處理瞬時(shí)降低的 T 淋巴細(xì)胞亞群，NK 細(xì)胞和單核細(xì)胞無影響[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Glofitamab (0.3-100 μg/kg，單劑量靜脈注射) 可誘導(dǎo)食蟹猴體內(nèi)細(xì)胞因子 (IL-1Ra, IL-2, IL-5, IL-6, IL-8, IL-10, G-CSF, IFN-γ 和 TNF-α) 水平呈劑量依賴性升高[3]。
Glofitamab (0.5 mg/kg, 靜脈注射, 單劑量) 在小鼠中誘導(dǎo)早期和持久的 T 細(xì)胞結(jié)合和活性[5]。

Glofitamab (靜脈注射, 單次劑量) 在有或沒有 Obinutuzumab (Gpt: 50 mg/kg) 處理的獼猴中的藥代動(dòng)力學(xué)參數(shù) (MeSt: 機(jī)制研究；MTD: 最大耐受劑量)[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 號(hào)
性狀

液體

顏色

Colorless to light yellow

中文名稱

格菲妥單抗
運(yùn)輸條件

Shipping with dry ice.
儲(chǔ)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).
純度 & 產(chǎn)品資料

純度: 99.80%

參考文獻(xiàn)

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量   濃度   體積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
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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產(chǎn)品名稱：
Glofitamab
目錄號(hào)：
HY-P99024
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