AGS-16C3F is an antibody-drug conjugate (ADC) targeting ENPP3. It is composed of an Anti-ENPP3/CD203c Antibody linked to MonomethylauristatinF via a linker. AGS-16C3F exhibits antitumor activity and is applicable in research on metastatic renal cell carcinoma (mRCC).

AGS-16C3F exhibits potent antiproliferative activity against ROSA cells with high CD203c expression, demonstrating IC50 values of 1.1 nM, 2.73 nM, 109.9 nM, and 146.5 nM in ROSA KIT D816V, ROSA KIT D816V-Gluc, HMC-1.1, and HMC-1.2 cells, respectively, when applied at concentrations of 0.001-1350 nM over 96 hours. Furthermore, AGS-16C3F, within a concentration range of 0.5-100 nM and exposure times of 96-120 hours, induces apoptosis targeting tumor cells that express high levels of CD203c.

AGS-16C3F (1.4 mg/kg, administered intravenously every 4 days for a total of 4 doses) significantly reduced tumor burden and prolonged survival in a NOD-SCID γ mouse model transplanted with ROSA KIT D816V-Gluc cells, without causing noticeable toxicity.