Биологическая активность
ARD2128 is a highly мощный, orally bioavailable PROTAC androgen рецептор (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
Оригинал на английском
ARD2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
Химические свойства
- CAS №
- 2222111-87-5
- Брутто-формула
- C₄₅H₅₀ClN₇O₆
- Мол. масса
- 820.37 г/моль
- SMILES
- ClC1=C(C#N)C([H])=C([H])C(=C1[H])OC1([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])(C1(C([H])([H])[H])C([H])([H])[H])N([H])C(C1C([H])=C([H])C(=C([H])C=1[H])N1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C1([H])C([H])([H])C([H])([H])N(C2C([H])=C([H])C3C(N(C4([H])C(N([H])C(C([H])([H])C4([H])[H])=O)=O)C(C=3C=2[H])=O)=O)C([H])([H])C1([H])[H])=O
- Синонимы
- N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-
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 Publication: [1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00882.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.