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

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].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

Human

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^[1].
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^[1].
Ulocuplumab (200 nM; 6 h) leads to induction of programmed cell death (PCD) is caspase independent^[1].
Ulocuplumab (10 μg/mL; 4 h) induces cell death via production of reactive oxygen species (ROS) in CLL cells^[1].
Ulocuplumab inhibits CXCL12-induced calcium flux with an EC₅₀ value of 10 nM in Ramos^[2].

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

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^[1].

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

7852  [NCBI]

P61073

ELISA, FACS, Functional assay

Unconjugated

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

144.84 kDa

1375830-34-4

Liquid

Colorless to light yellow

[Ulocuplumab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG4 kappa

• 
  Immobilized Human CXCR4/CD184 (Full Length) Protein-VLP can bind Ulocuplumab. The EC₅₀ for this effect is 36.64 ng/mL.
• 
  Flow cytometric analysis of 1.5×10⁶ THP-1 cells with Ulocuplumab (HY-P99272, red). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG4 (S228P) kappa Isotype Control (HY-P99003, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).

• [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.  [Content Brief]

  [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.  [Content Brief]