Биологическая активность
Dalpiciclib (SHR-6390) is a highly селективный, orally bioavailable CDK4/6 ингибитор with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts мощный antitumor activity in esophageal squamous клетка carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 клетка cycle arrest.
Оригинал на английском
Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.
Химические свойства
- CAS №
- 1637781-04-4
- Брутто-формула
- C₂₅H₃₀N₆O₂
- Мол. масса
- 446.56 г/моль
- SMILES
- O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(C4CCNCC4)C=C3)N=C2N1C5CCCC5
- Синонимы
- SHR-6390; SHR6390; SHR 6390; Dalpiciclib
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]. Zhang P, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021;9(1):24. Published 2021 Apr 12. [2]. Wang J, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017;15(1):127. Published 2017 Jun 2.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.