Биологическая активность
Rasarfin is a novel dual Ras and ARF6 ингибитор. Rasarfin blocks агонист-mediated internalization of AT1R and other GPCRs. Rasarfin also potently inhibits агонист-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer клетка proliferation. In silico modeling and in vitro studies reveal a unique связывание modality of Rasarfin within the SOS-связывание domain of Ras. Rasarfin is a novel dual Ras and ARF6 ингибитор. Rasarfin blocks агонист-mediated internalization of AT1R and other GPCRs. Rasarfin also potently inhibits агонист-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer клетка proliferation. In silico modeling and in vitro studies reveal a unique связывание modality of Rasarfin within the SOS-связывание domain of Ras.
Оригинал на английском
Rasarfin is a novel dual Ras and ARF6 inhibitor. Rasarfin blocks agonist-mediated internalization of AT1R and other GPCRs. Rasarfin also potently inhibits agonist-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer cell proliferation. In silico modeling and in vitro studies reveal a unique binding modality of Rasarfin within the SOS-binding domain of Ras. Rasarfin is a novel dual Ras and ARF6 inhibitor. Rasarfin blocks agonist-mediated internalization of AT1R and other GPCRs. Rasarfin also potently inhibits agonist-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer cell proliferation. In silico modeling and in vitro studies reveal a unique binding modality of Rasarfin within the SOS-binding domain of Ras.
Химические свойства
- CAS №
- 674359-73-0
- Брутто-формула
- C₂₃H₂₄ClN₃O₃
- Мол. масса
- 425.15 г/моль
- SMILES
- O=C(C1=CC2=CC=CC=C2O1)NC3=CC=C(N4CCN(C(C(C)C)=O)CC4)C(Cl)=C3
- Синонимы
- Rasarfin
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.