Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) 是一种完全人 IgG4 抗CXCR4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。
| 生物活性 | Ulocuplumab (Anti-HumanCXCR4Recombinant Antibody/BMS-936564/MDX1338) is a fully humanIgG4anti-CXCR4antibody. Ulocuplumab inducesapoptosisand inhibits CXCL12 mediatedCXCR4activation-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] | |
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]。
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 IC50value of 1.9 nM and showed pro-apoptotic with an IC50value of 12.43 nM in primary leukemia cells from CLL patients. |
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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]。
| 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. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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