Eftozanermin alfa
Based on 1 publication(s) in Google Scholar
Eftozanermin alfa (ABBV-621) is a tumor necrosis factor-related apoptosis-inducing ligand receptor (TRAIL-R) agonist. Eftozanermin alfa is a fusion protein consisting of a mutant immunoglobulin G1-Fc linked to 2 single-chain trimers of TRAIL. Eftozanermin alfa induces apoptosis in tumor cells by activation of death receptors (DR4 receptor and DR5 receptor) with Kds of 780 nM and 635 nM. Eftozanermin alfa can be used for the research of multiple solid and heme malignancies.
For research use only. We do not sell to patients.
- Purity: 98.86%
- CAS No.: 1820660-69-2
- Molecular Weight:167.52 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Eftozanermin alfa
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Biological Activity
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Caspase-3 |
Caspase-7 |
Caspase-8 |
Eftozanermin alfa demonstrates a highly significant synergistic effect when combined with Venetoclax (HY-15531) in acute myeloid leukemia cell lines and proteasome inhibitors (Bortezomib (HY-10227) or Carfilzomib (HY-10455))[1][2].
Eftozanermin alfa (0-1 nM, 24 h) has a killing effect on 36% (45/126) of human solid tumor cells through the apoptosis pathway (increase in caspase-3/7/8 activity)[1][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Eftozanermin alfa (5 mg/kg, i.p., every other day for 5 days) demonstrates significant and broad anti-tumor activity in patient-derived xenograft (PDX) mice models[3].
Eftozanermin alfa (0.3-30 mg/kg, i.p., every other day for 5 days) exhibits clear dose-dependent anti-tumor activity against colorectal and breast cancer in mice[3].
Eftozanermin alfa (3-15 mg/kg, i.p., once every two days or 2-5 times a week) demonstrates significantly superior antitumor efficacy when combined with either Irinotecan (HY-16562), Docetaxel (HY-B0011), A-1331852 (HY-19741) compared to any single agent alone in mice[3].
Eftozanermin alfa (4-100 mg/kg, i.v., once weekly for 5 weeks) exhibits favorable pharmacokinetic profile and a wide therapeutic window in cynomolgus monkey[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SKM-1 induced xenograft model established in female CB-17 SCID (SKM-1) mice or female SCID-beige (MV-4-11 and OCI-AML2) mice[1]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection (i.p.), every other day for 5 days
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Result:Induced robust single-agent antitumor activity with complete regression of SKM-1 tumors.
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Animal Model:PDX model established in female SCID and SCID-Beige mice[3]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection (i.p.), every other day for 5 days
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Result:Demonstrated significant and broad anti-tumor activity in a wide range of PDX models, with efficacy independent of patient treatment history or tumor sample origin (primary vs. metastatic).
Was particularly active in colorectal cancer (CRC) and pancreatic cancer (PaCa).
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Animal Model:CRC PDX models (e.g., CTG-0064, CTG-0069) and pancreatic cancer PDX models (e.g., PA20, PA55, PA117) established in female SCID and SCID-Beige mice[3]
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Dosage:0.3, 1, 3, 10 and 30 mg/kg
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Administration:Intraperitoneal injection (i.p.), every other day for 5 days
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Result:Exhibited clear dose-dependent antitumor activity.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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[Homo sapiens TNFSF10 (TNF superfamily member 10, tumor necrosis factor (ligand)superfamily, member 10)]2-Homo sapiens IGHG1 Fc (Fragment constant)
ELISA, FACS, Functional assay
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Immobilized Human DR5/TRAIL R2 Protein (His Tag) can bind Eftozanermin alfa. The EC50 for this effect is 4.94 ng/mL.
Chemical Information
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CAS No. 1820660-69-2
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Appearance Liquid
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Molecular Weight 167.52 kDa
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Color Colorless to light yellow
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SMILES
[Eftozanermin alfa]
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Synonyms
ABBV-621
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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
Purity & Documentation
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Data Sheet (264 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
[1]. Tahir SK, et al. Activity of eftozanermin alfa plus venetoclax in preclinical models and patients with acute myeloid leukemia. Blood. 2023 Jan 30:blood.2022017333. [Content Brief]
[3]. Phillips DC, et al. Hexavalent TRAIL Fusion Protein Eftozanermin Alfa Optimally Clusters Apoptosis-Inducing TRAIL Receptors to Induce On-Target Antitumor Activity in Solid Tumors. Cancer Res. 2021 Jun 15;81(12):3402-3414. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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