Aprutumab
Based on 1 Customer Validation
Aprutumab (BAY 1179470) is a fully human fibroblast growth factor receptor 2 (FGFR2)-specific monoclonal antibody. Aprutumab induces FGFR2 endocytosis and degradation in cancer cells expressing FGFR2. Aprutumab serves as the targeted monoclonal antibody component of the antibody-drug conjugate BAY 1187982 (HY-141600) and mediates the endocytosis of the antibody-drug conjugate into FGFR2-positive cells. Aprutumab can be used for the research of FGFR2-positive solid tumors, including studies on gastric cancer and triple-negative breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 1634620-63-5
- Molecular Weight:144.6 kDa
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Human IgG1 lambda2
Human
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FGFR2-IIIb |
FGFR2-IIIc |
Aprutumab specifically binds to human FGFR2 protein with a Kd value of 75 nM[1].
Aprutumab binds to FGFR2 proteins from multiple non-human species (mouse, rat, dog, pig, rhesus monkey) with an EC50 of 0.25-0.35 nM[1].
Aprutumab (5-24 h) specifically induces FGFR2 internalization in FGFR2-positive SUM-52PE and SNU-16 cancer cells, but exerts no such effect in FGFR2-negative MDA-MB-231 cells[1].
Aprutumab (10 μg/mL; 5 h) reduces FGFR2 expression on the surface of SNU-16 gastric cancer cells, confirming antibody-induced endocytosis[1].
Aprutumab (6 h) colocalizes with early endosome (Rab7) and lysosome (LAMP1) markers in approximately 60% of viable SUM-52PE cells, indicating that it is transported to lysosomes for degradation[1].
After conjugation to form BAY 1187982, Aprutumab retains its binding affinity for the FGFR2 antigen, with an EC50 of 0.29 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 lambda
ELISA, FACS, Functional assay
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Loaded Aprutumab on AHC2 biosensor, can bind FGFR-2 alpha (IIIc) Protein, Human (Biotinylated, HEK293, His-Avi, HY-P78131) with an affinity constant of 1.819E-08 M as determined in BLI assay.
Chemical Information
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CAS No. 1634620-63-5
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Appearance Liquid
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Molecular Weight 144.6 kDa
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Color Colorless to light yellow
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SMILES
[Aprutumab]
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Synonyms
BAY 1179470
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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 (258 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)