NOTA -FZCD-3 is a NOTA -labeled FZCD-3 polypeptide precursor that targets cathepsin D ( CTSD ) with a K D of 0.65 μM. NOTA -FZCD-3 binds specifically to the active site of CTSD, exhibits rapid in vivo clearance properties, and remains stable in blood for more than 2 h. NOTA -FZCD-3 can be used in studies monitoring CTSD-positive tumors [1].
In Vivo, [68Ga]Ga-NOTA-FZCD-3 (3.7-7.4 MBq; intravenous injection; single administration) achieves sustained tumor uptake in MDA-MB-415 breast cancer xenografts, with an initial uptake of 3.20% ID/g at 0.5 h post-injection[1]. [68Ga]Ga-NOTA-FZCD-3 (2.5-7.4 MBq; intravenous injection; single administration) exhibits the highest tumor uptake rate and contrast in the MDA-MB-175VII breast cancer xenograft model, with a peak tumor-to-non-tissue ratio of 7.65 at 1 h post-injection[1]. [68Ga]Ga-NOTA-FZCD-3 (3.7-7.4 MBq; intravenous injection; single dose) achieves specific tumor uptake in A549 lung cancer xenografts, with an initial uptake of 2.47% ID/g at 0.5 h post-injection[1]. The uptake of [68Ga]Ga-NOTA-FZCD-3 (2.5-3.7 MBq; intravenous injection; single administration) in MDA-MB-175VII tumor xenografts is directly correlated with endogenous CTSD expression levels[1]. [68Ga]Ga-NOTA-FZCD-3 (intravenous injection; single dose) exhibits favorable biosafety in tumor-bearing BALB/c nude mice, with no organ toxicity detected 7 days post-injection[1].
In Vitro, [68Ga]Ga-NOTA-FZCD-3 (0.5-2 h; 37°C) remains stable for at least 2 hours at 37°C in normal saline and human serum, with no decomposition detected[1]. [68Ga]Ga-NOTA-FZCD-3 (0.5-2 h) is taken up by human breast cancer cell lines MCF-7, MDA-MB-468, MDA-MB-415 and MDA-MB-175VII in a time-dependent manner. The uptake level is directly correlated with endogenous CTSD expression, and a peak uptake rate of 1.45% is observed in MDA-MB-175VII cells at 1 h[1].
References:
[1]. Xi Y, et al. Design and Preclinical Evaluation of First 68Ga-Labeled Cathepsin D-Targeted Radiotracers. J Med Chem. 2025 Dec 11;68(23):25143-25156.
In Vivo, [68Ga]Ga-NOTA-FZCD-3 (3.7-7.4 MBq; intravenous injection; single administration) achieves sustained tumor uptake in MDA-MB-415 breast cancer xenografts, with an initial uptake of 3.20% ID/g at 0.5 h post-injection[1]. [68Ga]Ga-NOTA-FZCD-3 (2.5-7.4 MBq; intravenous injection; single administration) exhibits the highest tumor uptake rate and contrast in the MDA-MB-175VII breast cancer xenograft model, with a peak tumor-to-non-tissue ratio of 7.65 at 1 h post-injection[1]. [68Ga]Ga-NOTA-FZCD-3 (3.7-7.4 MBq; intravenous injection; single dose) achieves specific tumor uptake in A549 lung cancer xenografts, with an initial uptake of 2.47% ID/g at 0.5 h post-injection[1]. The uptake of [68Ga]Ga-NOTA-FZCD-3 (2.5-3.7 MBq; intravenous injection; single administration) in MDA-MB-175VII tumor xenografts is directly correlated with endogenous CTSD expression levels[1]. [68Ga]Ga-NOTA-FZCD-3 (intravenous injection; single dose) exhibits favorable biosafety in tumor-bearing BALB/c nude mice, with no organ toxicity detected 7 days post-injection[1].
In Vitro, [68Ga]Ga-NOTA-FZCD-3 (0.5-2 h; 37°C) remains stable for at least 2 hours at 37°C in normal saline and human serum, with no decomposition detected[1]. [68Ga]Ga-NOTA-FZCD-3 (0.5-2 h) is taken up by human breast cancer cell lines MCF-7, MDA-MB-468, MDA-MB-415 and MDA-MB-175VII in a time-dependent manner. The uptake level is directly correlated with endogenous CTSD expression, and a peak uptake rate of 1.45% is observed in MDA-MB-175VII cells at 1 h[1].
References:
[1]. Xi Y, et al. Design and Preclinical Evaluation of First 68Ga-Labeled Cathepsin D-Targeted Radiotracers. J Med Chem. 2025 Dec 11;68(23):25143-25156.