Биологическая активность
DOTA-NI-FAPI-04 is a FAP ингибитор (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact.
Оригинал на английском
DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact.
Химические свойства
- Брутто-формула
- C₅₁H₆₉F₂N₁₅O₁₄
- Мол. масса
- 1154.18 г/моль
- SMILES
- O=C(CN1CCN(CCN(CCN(CC1)CC(O)=O)CC(O)=O)CC(N[C@@H](CCC(NCCCN2C=CN=C2[N+]([O-])=O)=O)C(N3CCN(CCCOC4=CC=C(C5=C4)N=CC=C5C(NCC(N6[C@@H](CC(F)(C6)F)C#N)=O)=O)CC3)=O)=O)O
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.