Биологическая активность
KRCT-6j is a мощный and селективный TYRO3 ингибитор, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated клетка migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.
Оригинал на английском
KRCT-6j is a potent and selective TYRO3 inhibitor, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated cell migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.
Химические свойства
- CAS №
- 2250085-28-8
- Брутто-формула
- C₂₀H₂₂Cl₂N₆
- Мол. масса
- 417.33 г/моль
- SMILES
- C1CCCC(NC2C(C3C=NN(C)C=3)=CN=C(N=2)NC2=CC(Cl)=CC(=C2)Cl)C1
- Синонимы
- KRCT-6j; N4-Cyclohexyl-N2-(3,5-dichlorophenyl)-5-(1-methyl-1H-pyrazol-4-yl)-2,4-pyrimidinediamine
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.