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CAS No. : 1375830-34-4
MCE 国际站:Ulocuplumab
产品活性: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。
研究领域:GPCR/G Protein | Immunology/Inflammation
作用靶点:CXCR
In Vitro: Ulocuplumab (0-100 μM; 48 h) lacks antibody dependent cellular cytotoxicity (ADCC) or complement (CDC) activity, but also induces apoptosis mediated by CXCR4 binding in Ramos cells and CLL/cancer cell lines, also shows pro-apoptotic in primary leukemia cells from CLL patients.
Ulocuplumab (0.2 μM and 2 μM; 15 s) inhibits F-actin polymerization and reduces the peak response to CXCL12, and also (20 nM-2 μM; 1 h) inhibits cell migration.
Ulocuplumab (200 nM; 6 h) leads to induction of programmed cell death (PCD) is caspase independent.
Ulocuplumab (10 μg/mL; 4 h) induces cell death via production of reactive oxygen species (ROS) in CLL cells.
Ulocuplumab inhibits CXCL12-induced calcium flux with an EC50 value of 10 nM in Ramos.
In Vivo: Ulocuplumab (3-30 mg/kg; i.p.; every 3-4 days for 5 doses; 65 days in total) inhibits tumor growth of multiple myeloma xenograft models in mice, including Ramos B cells, HL-60 cells, MOLP-8 cells, Nomo-1 cells, and JJN-3R cells models.
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