Биологическая активность
GSK3830052 is a novel DNMT1-селективный ингибитор (IC50 = 0.11 ± 0.02 µM). In in vitro assays, compounds in this series, including GSK3830052, inhibit human DNMT1 activity selectively over DNMT3A/3B, produce robust DNA hypomethylation, and trigger transcriptional reactivation and anti‑proliferative effects in leukemia клетка lines at low‑micromolar concentrations. In animal models, analogs of this series achieve significant tumor regression and survival benefit in acute myeloid leukemia xenografts with improved tolerability compared to decitabine, demonstrating dose‑dependent antitumor efficacy with reduced hematologic toxicity, although specific numeric IC₅₀/ED₅₀ values for GSK3830052 alone aren’t detailed in the open article.
Оригинал на английском
GSK3830052 is a novel DNMT1-selective inhibitor (IC50 = 0.11 ± 0.02 µM). In in vitro assays, compounds in this series, including GSK3830052, inhibit human DNMT1 activity selectively over DNMT3A/3B, produce robust DNA hypomethylation, and trigger transcriptional reactivation and anti‑proliferative effects in leukemia cell lines at low‑micromolar concentrations. In animal models, analogs of this series achieve significant tumor regression and survival benefit in acute myeloid leukemia xenografts with improved tolerability compared to decitabine, demonstrating dose‑dependent antitumor efficacy with reduced hematologic toxicity, although specific numeric IC₅₀/ED₅₀ values for GSK3830052 alone aren’t detailed in the open article.
Химические свойства
- CAS №
- 2170141-06-5
- Брутто-формула
- C₂₂H₂₈N₆O₂S₂
- Мол. масса
- 472.63 г/моль
- SMILES
- CS(=O)(N(C1=CC=C(CSC2=NC(N(C)CCNC)=C(C#N)C(CC)=C2C#N)C=C1)C)=O
- Синонимы
- GSK3830052; GSK 3830052; GSK-3830052
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.