1. GPCR/G Protein Neuronal Signaling NF-κB
  2. Orexin Receptor (OX Receptor) NF-κB
  3. BGB-A445

BGB-A445 是一种人源化非配体阻断型激动性的 OX40 单克隆抗体,对 OX40 具有高亲和力。BGB-A445 可激活下游 NF-κB 通路,诱导免疫细胞的活化、增殖和存活。BGB-A445 可通过抗体依赖的细胞毒性作用 (ADCC),以剂量依赖性的方式显著消耗调节性 T 细胞。BGB-A445 在 MC38 小鼠模型中显示出强大的、剂量依赖性的抗肿瘤功效。BGB-A445 可用于癌症研究,如结肠腺癌。

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BGB-A445 Chemical Structure

BGB-A445 Chemical Structure

CAS No. : 3033874-57-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BGB-A445 is a humanized non-ligand-blocking agonistic OX40 monoclonal antibody with high affinity to OX40. BGB-A445 activates downstream NF-κB pathway to induce immune cell activation, proliferation, and survival. BGB-A445 dose-dependently and significantly depletes regulatory T cells via antibody-dependent cellular cytotoxicity (ADCC). BGB-A445 demonstrates robust and dose-dependent antitumor efficacy in the MC38 mice models. BGB-A445 can be used for the researches of cancer, such as colon adenocarcinoma[1][2].

IC50 & Target

TNFRSF4/OX40/CD134

体外研究
(In Vitro)

BGB-A445 (0.01-10 µg/mL, 1 h) 以剂量依赖的方式与细胞表面过表达的 OX40 紧密结合,在 HuT78 细胞中的 EC50 值为 0.219 µg/mL,在原代人 CD4 阳性的 T 细胞中的 EC50 值为 0.157 µg/mL[1]

BGB-A445 (0-10 µg/mL, 48 h) 通过上调 DC (dendritic cell) 成熟/激活标志物 CD83 和 CD86 的水平诱导 DC 细胞成熟[1]

BGB-A445 (0.0001-10 µg/mL, 48 h) 以剂量依赖的方式增加 HuT78/OX40 细胞 (EC50 值为 0.059 µg/mL) 和原代 CD4 阳性的 T 细胞中 IL-2 的产生[1]

BGB-A445 (0.001-10 µg/mL, overnight) 诱导针对 OX40 水平高且 OX40 表达细胞百分比高的肿瘤调节性 T 细胞的抗体依赖的细胞介导的细胞毒性作用 (ADCC)[1]

BGB-A445 (0.001-10 µg/mL, overnight) 可增加 PBMCs 中 T 细胞中 CD8 阳性细胞的百分比,同时降低调节性 T 细胞的百分比[1]

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

体内研究
(In Vivo)

BGB-A445 (0.3-10 mg/kg, i.p. weekly for 2-4 times) 在 MC38、CT26WT 和 PAN02 同基因小鼠模型中显示出强大的抗肿瘤活性,并以剂量依赖性方式增加效应 T 细胞的增殖[1][2]

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

Animal Model: MC38 tumor mice model[1]
Dosage: 0.3, 1, 3 and 10 mg/kg
Administration: Intraperitoneal injection, weekly for 2 times
Result: Dose-dependently increased the number of CD4 Teffs, CD8 T cells and proliferating (Ki67+) Teffs, including CD4 T effector cells (CD3+CD4+FOXP3−) andCD8 T cells (CD3+CD8+).
Demonstrated significantly more potent activation in promoting the proliferation of CD8 T cells and memory phenotype CD8 T cells.
Dose-dependently increased the CD8+/Treg ratios.
Animal Model: MC38 syngeneic model[1]
Dosage: 0.4, 2, and 10 mg/kg
Administration: Intraperitoneal injection, weekly for 2 times
Result: Showed dose-dependent antitumor efficacy with the TGI rates of 14%, 80%, and 78%, respectively.
Animal Model: Anti-PD1-resistant PAN02 syngeneic model[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection, once a week for about 32 days
Result: Achieved a TGI rate of 75% by day 32 and showed no reduction of body weight at 3 mg/kg.
Animal Model: CT26WT tumor model[2]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection, once a week for about 28 days
Result: Suppressed the tumor growth.
基因 ID

7293  [NCBI]

Accession
靶点

TNFRSF4/OX40/CD134

应用

ELISA, FACS, Functional assay

偶联物

Unconjugated

复溶方法

The product can be reconstituted/diluted with sterile PBS or saline.

CAS 号
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
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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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产品名称:
BGB-A445
目录号:
HY-P991613
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