Etaracizumab
Based on 1 publication(s) in Google Scholar
Etaracizumab (LM 609) is an αvβ3 integrin IgG mAb. Etaracizumab is developed to target αvβ3+ 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 ofαvβ3-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).
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 892553-42-3
- Molecular Weight:146.64 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Etaracizumab
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Biological Activity
Human IgG1 kappa
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Orthotopic mouse model of advanced ovarian cancer in three cell lines (SKOV3ip1, A2780ip2, and Hey8)[4]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice per week
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Result:Reduced tumor growth by 48.8% compared to IgG control in the SKOV3ip1 model.
Significantly reduced tumor growth by 83.3% when combined with Paclitaxel (HY-B0015) compared to control IgG alone in the SKOV3ip1 model.
Significantly reduced tumor growth by 86.4% when combined with Paclitaxel compared to control in the A2780ip2 model.
Significantly reduced tumor weight by 35.6% in the HeyA8 model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG1 kappa
ELISA, FACS, Functional assay
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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.
Chemical Information
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CAS No. 892553-42-3
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Appearance Liquid
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Molecular Weight 146.64 kDa
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Color Colorless to light yellow
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SMILES
[Etaracizumab]
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Synonyms
LM609; MEDI-522
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Toxicol Appl Pharmacol
Ginkgolide B inhibits non-small cell lung cancer cells by modulating the integrin β3 pathway. [Abstract]2026 Jun:511:117806. PMID: 41921594
Purity & Documentation
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Data Sheet (262 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)