Anti-CD49B [GBR500 (Vatelizumab, TMC-2206)]

Absolute Antibody

Anti-CD49B [GBR500 (Vatelizumab, TMC-2206)]

9

This antibody binds an epitope in the domain I region of human alpha2 integrin. This epitope spans a region encompassing amino acid residues, K40, N73, Q89, Y93, R165, and N166 and optionally, other amino acid residues of the alpha2 integrin I domain. Thi

The binding of this antibody to recombinant GST-human alpha2I domain fusion protein and intact alpha2beta1 integrin was evaluated using ELISA. It was reported that this antibody bound immobilized human alpha2beta1 integrin with a binding affinity in the nanomolar range. The reactivity of this antibody towards alpha2beta1 integrin expressed on blood cells from different species was evaluated by flow cytometry (US7807794). In vitro, this antibody inhibits the binding of PC3 prostate cancer cells to collagen with an EC50 of 0.035 microg/ml. To study the impact of VLA-2 on extravasation in a PC3-luc metastasis model, this antibody was used to block VLA-2 before injection of tumor cells and by pre-dosing mice with a 50 mg/kg dose i.v. Bi-weekly treatment with this antibody at 5 mg/kg successfully slowed tumor growth and was as effective as bevacizumab 5 mg/kg treatment (Attinger et al., Cancer Research 2011). A study involving orthotopic mouse xenograft model used a DU145-luc cell line and explored the importance of VLA-2 for tumor growth in a physiological setting. It was reported that VLA-2 inhibition leads to modest growth reduction in subcutaneous xenografts (Hou et al., Mol Cancer Ther 2011). In a phase 2 clinical study in multiple sclerosis patients, the safety and efficacy of this antibody was evaluated. Following treatment with this antibody enhanced frequencies of regulatory T cells (TREG) were reported (PMID: 30783682).

Flow Cytometry, ELISA, Neutralisation/Blocking

Research Use Only

Monoclonal

GBR500 (Vatelizumab, TMC-2206)

ITGA2

integrin subunit alpha 2

alpha 2 subunit of VLA-2 receptor; BR; CD49 antigen-like family member B; CD49B; collagen receptor; GPIa; HPA-5; human platelet alloantigen system 5; integrin alpha-2; integrin, alpha 2 (CD49B, alpha 2 subunit of VLA-2 receptor); platelet antigen Br; platelet glycoprotein GPIa; platelet membrane glycoprotein Ia; very late activation protein 2 receptor, alpha-2 subunit; VLA-2; VLAA2

Mouse

IgG2a

Integrin alpha-2

Human, Monkey, Primate, Rat

-20°C,2°C to 8°C

12352203