Etaracizumab  (Synonyms: LM609; MEDI-522)

Etaracizumab (LM 609) is an α_vβ₃ integrin IgG mAb. Etaracizumab is developed to target α_vβ₃+ cancer cells via NK cell-mediated cytotoxicity. Etaracizumab sterically hinders access of large ligands to the RGD-binding pocket, without obstructing it. Etaracizumab decreases p-Akt in vitro. Etaracizumab can decrease cancer proliferation and invasion. Etaracizumab induces tumor cell apoptosis, and inhibition ofα_vβ₃-mediated cell adhesion, endothelial cell migration and osteoclast-mediated bone resorption. Etaracizumab can be studied in anti-tumor research against cancers such as ovarian cancer, metastatic melanoma as well as advanced solid tumors. Recommend Isotype Control: Human IgG1 kappa, Isotype Control (HY-P99001)^{[1][2][3][4][5]}.

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Human

Integrin aVb3

Etaracizumab (24 h) decreases the degree of p-Akt by 39% in the SKOV3ip1 cells^[4].
Etaracizumab (100 μg/mL, 5 d) significantly inhibits growth of ovarian cancer cells in the presence of Vitronectin (HY-P2452)-coating^[4].
Etaracizumab (1-10 μg/mL, 24 h) significantly inhibits ovarian cancer cell invasion^[4].

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

Etaracizumab (10 mg/kg, i.p., twice per week) inhibits tumor growth in orthotopic mouse model of ovarian cancer^[4].

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

3685  [NCBI] & 3690  [NCBI]

P06756 & P05106

ELISA, FACS, Functional assay

Unconjugated

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

146.64 kDa

892553-42-3

Liquid

Colorless to light yellow

[Etaracizumab]

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 IgG1 kappa

• 
  Flow cytometric analysis of 1X10⁶ HUVEC cells labeling Etaracizumab (HY-P99291, red). Cells were fixed with 4% paraformaldehyde. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Fluor 488-conjugated AffiniPure Goat Anti-Human IgG H&L (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa (HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
• 
  Immobilized Human Integrin αVβ3, His Tag&Tag Free can bind Etaracizumab. The EC₅₀ for this effect is 6.778 ng/mL.

• [1]. Hersey P, et al. A randomized phase 2 study of etaracizumab, a monoclonal antibody against integrin alpha(v)beta(3), + or - dacarbazine in patients with stage IV metastatic melanoma. Cancer. 2010 Mar 15;116(6):1526-34.  [Content Brief]

  [2]. Joshua P. Reddy, et al, Abstract 6358: Arming tumor-associated macrophages to inhibit cancer progression. Cancer Res 15 March 2024; 84 (6_Supplement): 6358.

  [3]. Delbaldo, C., et al., (2008). Phase I and pharmacokinetic study of etaracizumab (Abegrin), a humanized monoclonal antibody against alphavbeta3 integrin receptor, in patients with advanced solid tumors. Investigational new drugs, 26(1), 35–43.  [Content Brief]

  [4]. Landen, C. N., et al., (2008). Tumor-selective response to antibody-mediated targeting of alphavbeta3 integrin in ovarian cancer. Neoplasia (New York, N.Y.), 10(11), 1259–1267.  [Content Brief]

  [5]. Borst, A. J., et al., (2017). The Therapeutic Antibody LM609 Selectively Inhibits Ligand Binding to Human αVβ3 Integrin via Steric Hindrance. Structure (London, England : 1993), 25(11), 1732–1739.e5.  [Content Brief]