| Bioactivity | 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]. |
| Invitro | 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]。 Apoptosis Analysis[1] Cell Line: |
| 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]。 Animal Model: |
| Name | Ulocuplumab |
| CAS | 1375830-34-4 |
| Molar Mass | 146.2 (kDa) |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kashyap MK, et al. Ulocuplumab (BMS-936564 / MDX1338): a fully human anti-CXCR4 antibody induces cell death in chronic lymphocytic leukemia mediated through a reactive oxygen species-dependent pathway. Oncotarget. 2016 Jan 19;7(3):2809-22. [2]. Kuhne MR, et al. BMS-936564/MDX-1338: a fully human anti-CXCR4 antibody induces apoptosis in vitro and shows antitumor activity in vivo in hematologic malignancies. Clin Cancer Res. 2013 Jan 15;19(2):357-66. |