Биологическая активность
SRX3177 is a мощный, triple BRD4/PI3K/CDK4/6 ингибитор with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).SRX3177 is capable of targeting BRD4, PI3K and CDK4/6 simultaneously, induces apoptosis and клетка cycle arrest and has in vitro efficacy in mantle клетка lymphoma, hepatocellular carcinoma and neuroblastoma models.SRX3177 has antitumor efficacy in in vivo xenograft models and is less toxic than the combination of agents that inhibit individual targets.
Оригинал на английском
SRX3177 is a potent, triple BRD4/PI3K/CDK4/6 inhibitor with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).SRX3177 is capable of targeting BRD4, PI3K and CDK4/6 simultaneously, induces apoptosis and cell cycle arrest and has in vitro efficacy in mantle cell lymphoma, hepatocellular carcinoma and neuroblastoma models.SRX3177 has antitumor efficacy in in vivo xenograft models and is less toxic than the combination of agents that inhibit individual targets.
Химические свойства
- CAS №
- 2241237-51-2
- Брутто-формула
- C₃₁H₃₂N₆O₄S
- Мол. масса
- 584.69 г/моль
- SMILES
- C1(NC2=CC=C(C3C4OC(N5CCOCC5)=CC(=O)C=4SC=3)C=C2)=NC=C2C=C(C(N(C)C)=O)N(C3CCCC3)C2=N1
- Синонимы
- 7H-Pyrrolo[2,3-d]pyrimidine-6-carboxamide, 7-cyclopentyl-N,N-dimethyl-2-[[4-[5-(4-morpholinyl)-7-oxo-7H-thieno[3,2-b]pyran-3-yl]phenyl]amino]-
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.