1. GPCR/G Protein Immunology/Inflammation
  2. CXCR
  3. Ulocuplumab

Ulocuplumab  (Synonyms: BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody)

目录号: HY-P99272 纯度: 99.90%
COA

Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) 是一种完全人 IgG4CXCR4 抗体。Ulocplumab 诱导癌细胞凋亡 (apoptosis),能够抑制 CXCL12 介导的慢性淋巴细胞白血病 (CLL) 细胞在 CXCR4 激活下的迁移。Ulocplumab 在急性髓系白血病 (AML),非霍奇金淋巴瘤 (NHL) 和多发性骨髓瘤移植模型中显示抗肿瘤活性。

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Ulocuplumab Chemical Structure

Ulocuplumab Chemical Structure

CAS No. : 1375830-34-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models[1][2].

IC50 & Target[1][2]

CXCR4

 

体外研究
(In Vitro)

Ulocplumab (0-100 μM; 48 h) 缺乏抗体依赖的细胞细胞毒性 (ADCC) 或补体 (CDC) 活性,但也在 Ramos 细胞和 CLL 或癌细胞系中诱导 CXCR4 结合介导的凋亡,也在 CLL 患者的原发性白血病细胞中显示促凋亡[1]
Ulocplumab (0.2 μM, 2 μM; 15 s) 抑制 F-actin 聚合,降低对 CXCL12 的峰响应,(20 nM-2 μM; 1 h) 还抑制细胞迁移[1]
Ulocplumab (200 nM; 6 h) 具有独立于 caspase 的程序性细胞死亡 (PCD) 诱导作用[1]
Ulocplumab (10 μg/mL; 4 h) 在CLL细胞中通过产生活性氧 (ROS) 诱导细胞死亡[1]
Ulocplumab 抑制 CXCL12 诱导的钙通量,在 Ramos 中 EC50 为 10 nM [2]

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

Apoptosis Analysis[1]

Cell Line: Ramos cells and primary leukemia cells (from CLL patients)
Concentration: 0-100 μM
Incubation Time: 48 hours
Result: Induced apoptosis in Ramos cells with an IC50 value of 1.9 nM and showed pro-apoptotic with an IC50 value of 12.43 nM in primary leukemia cells from CLL patients.
体内研究
(In Vivo)

Ulocplumab (3-30 mg/kg; 腹腔注射; 3-4 天 5 次剂量; 共 65 天) 抑制小鼠多发性骨髓瘤异种移植瘤模型的肿瘤生长,包括带有 Ramos B 细胞、HL-60 细胞、MOLP-8 细胞、Nomo-1 细胞和 JJN-3R 细胞的肿瘤模型[1]

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

Animal Model: Severe combined immunodeficient (SCID) mice of AML model (MOLP-8 cells)[1]
Dosage: 3-30 mg/kg
Administration: Intraperitoneal injection; every 3-4 days for 5 doses; last for 65 days
Result: Significantly delayed mean tumor growth by 66% and 56% when compared with isotype control on day 25.
Clinical Trial
分子量

146.2 (kDa)

CAS 号
性状

液体

颜色

Colorless to light yellow

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

Ulocuplumab 相关分类

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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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