Elritercept
Based on 1 Customer Validation
Elritercept (KER-050) is a modified activin type IIA receptor ligand trap. Elritercept binds to and neutralizes TGF-β superfamily ligands, including TGF-β, activins (activins), GDF8, GDF11 , and GDFs, blocking ActRIIa-mediated signaling, inhibiting SMAD2/3 signaling, and rebalancing signaling. Elritercept can be used in research on myelodysplastic syndromes, myelofibrosis, MDS/MF-associated anemia, and acute myeloid leukemia.
For research use only. We do not sell to patients.
- Purity : 97.868%
- CAS No.: 2727114-26-1
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Species Reactivity
Human
|
TGF-β |
activins |
GDF8 |
GDF11 |
ActRIIa |
Smad2 |
Smad3 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C1498-GFP mouse AML cells
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Concentration:400 ng/mL (alone and in combination with ActA 100 ng/mL)
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Incubation Time:overnight pre-incubation; 4 h (migration assessment)
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Result:Migratory ability of the AML cells was significantly reduced.
AML cells pre-incubated with an ActA-containing combination showed significantly reduced migration compared with ActA-pre-incubated cells.
ActA-induced migration of AML cells was inhibited.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 9 weeks old)[6]
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Dosage:10 mg/kg
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Administration:intraperitoneal (IP) injection; twice weekly; 3 weeks
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Result:Increased RBCs (+21%), hemoglobin (+16%), hematocrit (+16%), and reticulocytes (+21%) compared to vehicle control.
Increased BM osteoblast (+81%) and BMSC (+23%) populations compared to vehicle control.
Did not change CFU-F numbers compared to vehicle control.
Increased CFU-ALP (+52%) compared to vehicle control.
Increased CFU-Ob (+36%) compared to vehicle control.
Did not change CFU-ADP numbers compared to vehicle control.
Increased osteoblast marker gene expression, osterix (Sp7) and osteocalcin (Ocn), with no changes in adipocyte marker gene expression compared to vehicle control.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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FPIA_[PROTEIN]2-FC
Application
ELISA, FACS, Functional assay
Verified Bioactivity
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Immobilized Activin A Protein, Human (Biotinylated, HEK293, Avi, HY-P703994) can bind Elritercept. The EC50 for this effect is 9.269 ng/mL.
Chemical Information
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CAS No. 2727114-26-1
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Appearance Liquid
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Color Colorless to light yellow
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Synonyms
KER-050
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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 (264 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)