Recombinant Human IGF1, partial (Active) corresponds to the Gly49-Ala118 fragment of the mature IGF1 protein (70 amino acids, 7.6 kDa) and retains three intramolecular disulfide bonds essential for structural stability and receptor binding . Produced in E. coli, it achieves >98% purity with low endotoxin levels (<1 EU/μg) .
Parameter | Specification |
---|---|
Amino Acid Range | Gly49-Ala118 |
Expression System | Escherichia coli |
Purity | >98% (SDS-PAGE) |
Activity (ED₅₀) | 0.3–1.5 ng/mL (MCF-7 cell proliferation) |
This recombinant fragment binds IGF1R with high affinity, activating downstream pathways such as PI3K-AKT and Ras-MAPK, which regulate cell survival, glucose uptake, and growth . Key functions include:
Mitogenic Activity: Stimulates proliferation in breast cancer (MCF-7) and osteoblast cell lines at picomolar concentrations .
Metabolic Regulation: Enhances glucose transport in osteoblasts at 10–100x lower concentrations than insulin .
Cross-Species Reactivity: 94% sequence identity with murine IGF1 enables interspecies applications .
Dose-Dependent Kinetics: Nonlinear elimination observed at higher doses (80 μg/kg), attributed to saturation of IGF-binding proteins (IGFBPs) .
Dose (μg/kg) | Cₘₐₓ (μg/L) | AUC (ng·h/mL) |
---|---|---|
40 | 341 | 2,050 |
80 | 794 | 3,590 |
Growth Disorders: In a 12-month trial, 80 μg/kg/day increased height velocity from 3.8 cm/yr to 6.6 cm/yr in IGF1-deficient patients .
Rett Syndrome: Improved apnea frequency and anxiety scores in a phase 1 trial (40–120 μg/kg BID) .
Metabolic Dysregulation: Reduces insulin resistance by suppressing GH secretion and normalizing IGFBP levels .
IGF1 Deficiency Therapy: Subcutaneous administration (40–80 μg/kg) normalized circulating IGFBP-3 (+55%) and reduced GH peaks by 88%, correlating with lean mass gains .
Neurological Effects: In Rett syndrome, IGF1 crossed the blood-brain barrier (CSF levels: +32%) and reversed EEG markers of anxiety .
Cancer Research: Promoted tumor progression in vitro via AKT pathway activation, underscoring its dual role in therapy and oncogenesis .