1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. Zimberelimab

Zimberelimab  (Synonyms: GLS-010; AB-122; WBP-3055)

目录号: HY-P99109 纯度: 99.90%
COA

Zimberelimab (GLS-010) 是一种全人 IgG4PD-1 单克隆抗体,对人 PD-1EC50 为 210 pM。Zimberelimab 可有效阻断 CHO-S 细胞中 PD-L1 和 PD-L2 与细胞表面 PD-1 的结合,IC50 值分别为 580 pM 和 670 pM。Zimberelimab 具有抗肿瘤活性,可用于多种癌症研究,包括宫颈癌、非小细胞肺癌和经典霍奇金淋巴瘤。

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Zimberelimab Chemical Structure

Zimberelimab Chemical Structure

CAS No. : 2259860-24-5

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规格 价格 是否有货 数量
1 mg ¥2800
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5 mg ¥7200
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10 mg ¥11500
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Zimberelimab (GLS-010) is a fully human IgG4 anti-PD-1 monoclonal antibody with an EC50 of 210 pM for human PD-1. Zimberelimab effectively blocks the binding of PD-L1 and PD-L2 to cell-surface PD-1 in CHO-S cells, with IC50 values of 580 pM and 670 pM, respectively. Zimberelimab shows antitumor activities, and can be used for various cancers research, including cervical cancer, non-small cell lung cancer and classical Hodgkin’s lymphoma[1][2].

体外研究
(In Vitro)

Zimberelimab 对人 PD-1 的 EC50 为 210 pM,但不结合相关的 CD28 家族受体,例如 ICOS、CD28 和 CTLA-4[1]
Zimberelimab 与细胞表达的人 PD-1 结合,抑制受体与人 PD-L1 和 PD-L2 的相互作用,IC50 分别为 580 pM 和 670 pM[1 ]
Zimberelimab 剂量依赖性地增强 CD4+ T 细胞的 IFN-γ 产生和增殖,在浓度低于 100 pM 时达到饱和[1]

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

体内研究
(In Vivo)

Zimberelimab (10 and 20 mg/kg; i.v.; BIW*3) shows significant anti-tumor effects in mice[2].
PK parameters of Zimberelimab after single vd administrations of 2, 6, and 18 mg/kg in cynomolgus macaques[2]

PK parameters 2 mg/kg 6 mg/kg 18 mg/kg
C0 (mg/mL) 103 ± 23.7 (23.0%) 157 ± 18.7 (11.9%) 508 ± 48.0 (9.46%)
T1/2 (h) 111 ± 23.7 (30.5%) 115 ± 32.8 (28.5%) 129 ± 17.0 (13.1%)
Vss (mL/kg) 48.4 ± 7.48 (15.5%) 49.4 ± 6.49 (13.1%) 46.3 ± 5.49 (11.8%)
Cl (mL/h/kg) 0.288 ± 0.0373 (13.0%) 0.278 ± 0.0308 (11.1%) 0.183 ± 0.0293 (16.0%)
Tlast (h) 396 ± 141 (35.5%) 704 ± 203 (28.9%) 816 ± 0.00
AUC0-last (h*mg/mL) 6300 ± 1320 (21.0%) 21300 ± 2570 (12.1%) 98100 ± 16300 (16.6%)
AUCo‑inf (h*mg/mL) 7060 ± 1020 (14.5%) 21800 ± 2310 (10.6%) 101000 ± 16700 (16.6%)
MRT0-last (h) 126 ± 23.3 (18.4%) 164 ± 31.2 (19.0%) 236 ± 14.8 (6.27%)
MRT0-inf (h) 170 ± 29.7 (17.5%) 180 ± 29.4 (16.4%) 255 ± 17.4 (6.82%)
AUC0-inf/AUC0-last (%) 113 ± 11.8 (10.4%) 103 ± 0.940 (0.916%) 103 ± 0.940 (0.916%)

C0, initial drug concentration; T1/2, half-life; Vss, apparent volume of distribution in the steady-state; Cl, clearance; Tlast, the last time; AUC, area under the curve; MRT, mean residence time.

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

Animal Model: The human PD-1 knock-in mouse model of MC38 tumors[2]
Dosage: 10 and 20 mg/kg
Administration: Intravenous injection, BIW*3
Result: Showed statistically significant anti-tumor effects comparable with Pembrolizumab (HY-P9902).
Animal Model: Nine male and nine female cynomolgus monkeys[2]
Dosage: 2, 6, and 18 mg/kg
Administration: Intravenous injection (Pharmacokinetic Analysis)
Result: Displays long-term effects in cynomolgus monkeys, without differences between males and females.
Clinical Trial
CAS 号
性状

液体

颜色

Colorless to light yellow

中文名称

赛帕利单抗

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.

纯度 & 产品资料
参考文献

Zimberelimab 相关分类

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  • 稀释计算器

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  • 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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