1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  2. IGF-1R Akt
  3. Veligrotug

Veligrotug  (Synonyms: AVE1642; VRDN-001)

Cat. No.: HY-P990084 Purity: 99.25%
Technical Support

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.

CAS No. : 2728655-31-8

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Description

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[1][2].

Isotype

Human IgG1 kappa

Recommend Isotype Controls
Species Reactivity

Human

IC50 & Target

IGF1R/CD221

In Vitro

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.

ELISA Assay[2]

Cell Line: HepG2 cells
Concentration: 0.46-1000 nM
Incubation Time: 1 h preincubation at 37°C and 5% CO2
Result: Showed no significant antagonism of insulin-mediated IR phosphorylation in HepG2 cells at concentrations up to 1000 nM.
Parmacokinetics
Species Dose Route Cmax T1/2 Vss
Cynomolgus Monkey[2] 2 mg/kg i.v. 52.2 μg/mL 76.56 h 58.7 mL/kg
Cynomolgus Monkey[2] 10 mg/kg i.v. 243 μg/mL 130.08 h 74.2 mL/kg
Cynomolgus Monkey[2] 50 mg/kg i.v. 1080 μg/mL 171.6 h 107 mL/kg
In Vivo

Veligrotug (10-50 mg/kg; i.v.; weekly 30-minute infusion; 13 weeks) sustains an approximately 2.5-fold increase in serum IGF-1 concentrations in male and female cynomolgus monkeys throughout the dosing period, while the 2 mg/kg group loses this effect due to anti-drug antibody development in most animals[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cynomolgus monkeys (male and female, 2.0 to 2.9 years old, 1.6 to 2.2 kg)[2]
Dosage: 2 mg/kg; 10 mg/kg; 50 mg/kg
Administration: i.v.; weekly 30-minute infusion; 13 weeks
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.
Clinical Trial
Gene ID

3480  [NCBI]

Accession
Application

ELISA, FACS, Functional assay

Conjugated

Unconjugated

Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.

Molecular Weight

147.7 kDa

CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Veligrotug]

Shipping

Shipping with dry ice.

Formulation

Please refer to the lot-specific COA for specific buffer information.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Format
  • Human IgG1 kappa
Biological Activity
  • 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).
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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