Seribantumab
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Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models.
For research use only. We do not sell to patients.
- Purity: 96.043%
- CAS No.: 1334296-12-6
- Molecular Weight:143.14 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
Description
Isotype
Human IgG2 lambda
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
ERBB3/HER3
In Vitro
Seribantumab (0.1 nmol/L-10 μmol/L; 96 h) dose-dependently inhibits two cell lines that harbor NRG1 rearrangements (MDA-MB-175-VII, DOC4-NRG1 fusion and LUAD-0061AS3, SLC3A2-NRG1 fusion) with IC50 values of 0.02, 1.4, 45.2 and 203 μmol/L for MDA-MB-175-VII, LUAD-0061AS3, MCF-7 and HBECp53 cells, respectively[1]. Seribantumab (0.1, 1, and 10 μmol/L; 24-48 h) effectively inhibits growth of tumor cell lines that harbor NRG1 fusions or NRG1 amplification[1]. Seribantumab (0-0.5 μmol/L; 96 h) largely suppresses growth of NRG1-b1-stimulated MCF-7 cells[1]. Seribantumab (0-10 μmol/L; 48 h) induces apoptosis of cells harboring NRG1 rearrangements[1]. Seribantumab (0-10 μmol/L; 1 h) inhibits phosphorylation of downstream mediators in cells with NRG1 alterations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-175-VII and LUAD-0061AS3 cell lines
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Concentration:0-10 μmol/L
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Incubation Time:48 hours
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Result:Dose-dependently increased caspase 3/7 activity and induced apoptosis of NRG1 fusion-positive breast and lung cancer cell lines.
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Cell Line:LUAD-0061AS3 and HBECp53-CD74-NRG1 cell lines
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Concentration:0, 0.001, 0.01, 0.1, 1 and 10 μmol/L
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Incubation Time:1 hour
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Result:Inhibited the phosphorylation of EGFR, HER2, HER3, HER4, AKT and STAT3 in LUAD-0061AS3 cells. Completely inhibited HER3, AKT, p70S6K and STAT3, and reduced phosphorylation of HER2, EGFR and HER4 to a lesser extent in HBECp53-CD74-NRG1 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunocompromised mice with LUAD-0061AS3 PDX tumors implanted[1]
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Dosage:0.6, 0.75 and 1 mg
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Administration:Intraperitoneal injection; 0.6, 0.75 and 1 mg for once
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Result:Effectively reduced tumor growth of mice and time- and dose-dependently reduced phosphorylation of HER2, HER3, AKT, and ERK1/2. Induced the expression if proapoptotic protein, BIM.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG2 lambda
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized HER3 Protein, Human (HEK293, His, HY-P72625) can bind Seribantumab. The EC50 for this effect is 7.53 ng/mL. -
Flow cytometric analysis of 1X106 MCF-7 cells labeling Seribantumab (HY-P99268, 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 (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG2 lambda (HY-P991206, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black).
Chemical Information
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CAS No. 1334296-12-6
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Appearance Liquid
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Molecular Weight 143.14 kDa
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Color Colorless to light yellow
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SMILES
[Seribantumab]
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Synonyms
SAR 256212; MM 121
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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.
Purity & Documentation
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Data Sheet (262 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)