Products
Aprutumab Biosimilar Antibody-Drug Conjugate (FGFR2) for Research
Pre-Made Aprutumab biosimilar, Whole mAb ADC, Anti-FGFR2 Antibody: Anti-BBDS/BEK/BFR-1/CD332/CEK3/CFD1/ECT1/JWS/K-SAM/KGFR/TK14/TK25 therapeutic antibody is a biosimilar expressed by mammalian cell line as a benchmark reference therapeutic antibody for biological drug disovery items including cell culture, assay development, animal model development, PK/PD model development (Pharmacokinetics & Pharmacodynamic) and mechanism of action (MOA) research.
Aprutumab Ixadotin is an antibody-drug conjugate (ADC) directed against the fibroblast growth factor receptor type 2 (FGFR2) and conjugated to an as of yet unidentified toxin, with potential antineoplastic activity. Upon intravenous administration, aprutumab ixadotin binds to FGFR2.
Order Information
| Catalog No. | Package | Price(In USD) |
|---|---|---|
| GMP-Bios-ab-031-1mg | 1mg | |
| GMP-Bios-ab-031-10mg | 10mg | |
| GMP-Bios-ab-031-100mg | 100mg | |
| GMP-Bios-ab-031-xmg | ≥100mg |
Product Details
| Products Name (INN Index) | Pre-Made Aprutumab biosimilar, Whole mAb ADC, Anti-FGFR2 Antibody: Anti-BBDS/BEK/BFR-1/CD332/CEK3/CFD1/ECT1/JWS/K-SAM/KGFR/TK14/TK25 therapeutic antibody |
| INN Name | Aprutumab |
| Target | FGFR2 |
| Format | Whole mAb ADC |
| Derivation | Human |
| Species Reactivity | Human |
| CH1 Isotype | IgG1 |
| VD LC | Lambda |
| Highest_Clin_Trial (Jan '20) | Phase-I |
| Est. Status | Discontinued |
| 100% SI Structure | None |
| 99% SI Structure | None |
| 95-98% SI Structure | None |
| Year Proposed | 2016 |
| Year Recommended | 2017 |
| Companies | Bayer |
| Conditions Approved | na |
| Conditions Active | na |
| Conditions Discontinued | Solid tumours |
| Development Tech | na |
About target - FGFR2
1. Protein Fibroblast growth factor receptor 2
2. Gene FGFR2
3. Organism Homo sapiens (Human)
Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an essential role in the regulation of osteoblast differentiation, proliferation and apoptosis, and is required for normal skeleton development. Promotes cell proliferation in keratinocytes and immature osteoblasts, but promotes apoptosis in differentiated osteoblasts. Phosphorylates PLCG1, FRS2 and PAK4. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. FGFR2 signaling is down-regulated by ubiquitination, internalization and degradation. Mutations that lead to constitutive kinase activation or impair normal FGFR2 maturation, internalization and degradation lead to aberrant signaling. Over-expressed FGFR2 promotes activation of STAT1.
Catalytic activity
ATP + L-tyrosyl-[protein] = ADP + H+ + O-phospho-L-tyrosyl-[protein]
EC:2.7.10.1
Activity regulation
Present in an inactive conformation in the absence of bound ligand. Ligand binding leads to dimerization and activation by autophosphorylation on tyrosine residues. Inhibited by ARQ 523 and ARQ 069; these compounds maintain the kinase in an inactive conformation and inhibit autophosphorylation.
