Margetuximab

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Margetuximab 

Margetuximab 是一种嵌合抗 HER2 单克隆抗体,具有优化的 Fc 结构域,EC50 为 39.33 ng/mL。Margetuximab 可用于抗癌研究。

Margetuximab

Margetuximab Chemical Structure

CAS No. : 1350624-75-7

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生物活性

Margetuximab is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching anticancer[1].

IC50 & Target

EC50: 39.33 ng/mL (HER2)[1]

体外研究
(In Vitro)

Margetuximab enhances the antibody-dependent cell-mediated cytotoxicity activity of effector cells expressing the CD16A-158F variant[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: JIMT-1, MCF-7, ZR-75-1, SKBR-3, HT-29, SW750 and N87[1]
Concentration: 0.001-1000 ng/mL
Incubation Time: 6 days
Result: Enhances the antibody-dependent cell-mediated cytotoxicity activity of effector cells expressing the CD16A-158F variant.

体内研究
(In Vivo)

Margetuximab (2-4 mg/kg; IP 5 or 6 times at weekly) can firstly and significantly reduces the tumor size at day 30 – 37 in mice model[1].
Margetuximab (15-150 mg/kg; IV; 6 weekly) exhibits well tolerated in cynomolgus monkeys, decreases NK cells by an average of 51%, and induces IL-6 release[1].
Margetuximab (50 mg/kg; IV; single dosage) exhibits favorable safety profile[1].
Pharmacokinetic Parameters of Margetuximab in cynomolgus monkeys[1].

Male, IV (50 mg/kg) Female, IV (50 mg/kg)
Cmax (mg/mL) 1.62 ± 0.10 1.70 ± 0.14
AUC0-¥ (mg·hour/mL) 294.1 ± 53.2 314.2 ± 31.3
T1/2β (days) 9.3 ± 1.8 9.7 ± 1.1
Clearance (mL/hour) 0.43 ± 0.07 0.40 ± 0.04
VSS (mL) 132 ± 2 127 ± 8

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

CAS 号

1350624-75-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Nordstrom JL, et al. Anti-tumor activity and toxicokinetics analysis of MGAH22, an anti-HER2 monoclonal antibody with enhanced Fcγ receptor binding properties. Breast Cancer Res. 2011;13(6):R123. doi:10.1186/bcr3069

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