Veligrotug
Based on 1 Customer Validation
Veligrotug (AVE1642) is a selective, fully human IGF-1R antagonist antibody with a Kd value of 0.55 nM for hIGF-1R. Veligrotug blocks the phosphorylation of downstream AKT. Veligrotug is applicable to research related to thyroid eye disease.
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 2728655-31-8
- Molecular Weight:147.7 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
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Human IgG1 kappa
Human
IGF1R/CD221
Veligrotug binds to recombinant hIGF-1R ECD protein with high affinity, with a mean Kd value of 0.55 nM[2].
Veligrotug (30 min) binds with high affinity to HOCF cells endogenously expressing IGF-1R, with a mean EC50 of 2.41 nM and a mean Kd of 1.85 nM[2].
Veligrotug (0.46-1000 nM; 1 h) does not inhibit insulin-mediated insulin receptor phosphorylation in HepG2 cells even at concentrations as high as 1000 nM[2].
Veligrotug (0.008-500 nM; 30 min preincubation on ice) almost completely inhibits the binding of IGF-1 to IGF-1R on FreeStyle 293-F cells at concentrations ≥50 nM[2].
Veligrotug (0.0001-333 nM; 1 h) completely inhibits IGF-1-mediated AKT phosphorylation in primary HOCF cells at concentrations of 10-30 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0.46-1000 nM
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Incubation Time:1 h preincubation at 37°C and 5% CO2
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Result:Showed no significant antagonism of insulin-mediated IR phosphorylation in HepG2 cells at concentrations up to 1000 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys (male and female, 2.0 to 2.9 years old, 1.6 to 2.2 kg)[2]
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Dosage:2 mg/kg; 10 mg/kg; 50 mg/kg
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Administration:i.v.; weekly 30-minute infusion; 13 weeks
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Result:Induced an approximately 2.5-fold increase in IGF-1 concentrations for all dose groups following the first dose (Days 0-7).
Sustained elevated IGF-1 serum concentrations throughout the 13-week dosing period for the 10 and 50 mg/kg dose groups.
Maintained elevated IGF-1 concentrations during the recovery period for the 50 mg/kg dose group.
Saw IGF-1 concentrations return to baseline in 5 of 6 animals in the 2 mg/kg group, correlating with anti-drug antibody development.
| 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 MCF-7 cells labeling Veligrotug (HY-P990084, 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 IgG1 kappa (HY-P99001, 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. 2728655-31-8
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Appearance Liquid
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Molecular Weight 147.7 kDa
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Color Colorless to light yellow
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SMILES
[Veligrotug]
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Synonyms
AVE1642; VRDN-001
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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 (261 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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