Aprutumab  (Synonyms: BAY 1179470)

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^[1].

Human IgG1 lambda2

Human IgG1 lambda2, Isotype Control

Human

Aprutumab specifically binds to human FGFR2 protein with a K_d 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.

2263  [NCBI]

P21802

ELISA, FACS, Functional assay

Unconjugated

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

144.6 kDa

1634620-63-5

Liquid

Colorless to light yellow

[Aprutumab]

Shipping with dry ice.

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

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

• 
  Human IgG1 lambda

• 
  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.

• [1]. Sommer A, et al. Preclinical Efficacy of the Auristatin-Based Antibody-Drug Conjugate BAY 1187982 for the Treatment of FGFR2-Positive Solid Tumors. Cancer Res. 2016;76(21):6331-6339.  [Content Brief]