Aflibercept; Recombinant human VEGFRs, Fc tag

Specification

• Cat#: THP-0006
• Product Name: Aflibercept; Recombinant human VEGFRs, Fc tag
• Description: The product is a recombinant fusion protein that comprises of two main components: the vascular endothelial growth factor (VEGF) binding portions from the extracellular domains of human VEGF receptors 1 and 2 which is then fused to the Fc portion of human IgG1. Structurally, the product is a dimeric glycoprotein with a protein molecular weight of 96.9 kilo Daltons (kDa). It contains approximately 15% glycosylation to give a total molecular weight of 115 kDa. All five putative N-glycosylation sites on each polypeptide chain predicted by the primary sequence can be occupied with carbohydrate and exhibit some degree of chain heterogeneity, including heterogeneity in terminal sialic acid residues, except at the single unsialylated site associated with the Fc domain.
• Sequences: SDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG
• Species: Human
• Molecular Weight: 115KDa (with glycosylation)
• Source: CHO
• Purity: >99% by SDS-Page and HPLC analysis
• Cas No: 862111-32-8
• Formula: C4318H6788N1164O1304S32
• Endotoxin Level: <0.001 EU per 1 μg of the protein by the LAL method
• Biological Activity: 40 mg/ml
• Storage: Lyophilized protein should be stored at < -20°C, though stable at room temperature for 3 weeks. Reconstituted protein solution can be stored at 2-8 °C for 1 week. Aliquots of reconstituted samples are stable at < -20°C for 3 months.

Pharmaceutical Information

• Pharmaceutical Application: Aflibercept
• Applications: The opthalmic agent is used for the treatment of neovascular (wet) age-related mascular degeneration (AMD) and macular edema following central retinal vein occulsion (CRVO). The systemic injection, known as ziv-aflibercept, in combination with 5-fluorouracil, leucovorin, irinotecan-(FOLFIRI), is for the treatment of metastatic colorectal cancer that is resistant to or progressed following treatment with oxaliplatin.
• Examples of Clinical Use: Neovascular (wet) age-related mascular degeneration (AMD) and macular edema following central retinal vein occulsion (CRVO)
• Pharmacodynamics: Compared to other anti-VEGF drugs like bevacizumab and ranibizumab, the product has a higher binding affinity to VEGF-A (Kd = 0.5 pM).
• Mechanism of action: Ablibercept is a recombinant fusion protein that acts as a decoy receptor for the ligands, vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PIGF). It prevents these ligands to binding to endothelial receptors, VEGFR-1 and VEGFR-2, to suppress neovascularization and decrease vascular permeability. This ultimately will slow vision loss or the progression of metastatic colorectal cancer.
• Affected organisms: Humans and other mammals
• Targets: Target 1. Vascular endothelial growth factor A; Target 2. Placenta growth factor; Target 3. Vascular endothelial growth factor B