Биологическая активность
ETC-168 (ETC168) is a мощный, селективный MNK киназы ингибитор with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.ETC-168 acts as a MNK2-biased, dual-MNK ингибитор in cells.ETC-168 induced dose-dependent growth suppression and inhibited 50% of клетка viability at 5 uM in LPS141 and MESSA, ETC-168 treatment elicited a consistent increase of cells in G0/G1 phase among LPS141, LP6, and MESSA cells in a dose-dependent manner. ETC-168 decreased cells of S and G2/M phases, while no significant induction of sub-G1 cells.Inhibition of MNK1/2 by ETC-168 elevated the expression of MNK1/2 at both transcript and protein levels in soft tissue sarcoma (STS) cells.ETC-168 effectively suppressed both p-4E and клетка viability in MESSA cells, but not CGP57380 and eFT508.ETC-168 suppresseed phosphorylation of ribosomal protein S6 (RPS6) in sensitive STS клетка, decreased expression of E2F1, FOXM1, and WEE1.Inhibition of MCL1 via S63845 synergizes with ETC-168 against STS cells.
Оригинал на английском
ETC-168 (ETC168) is a potent, selective MNK kinase inhibitor with biochemical IC50 of 23 and 43 nM against MNK1 and MNK2, respectively.ETC-168 acts as a MNK2-biased, dual-MNK inhibitor in cells.ETC-168 induced dose-dependent growth suppression and inhibited 50% of cell viability at 5 uM in LPS141 and MESSA, ETC-168 treatment elicited a consistent increase of cells in G0/G1 phase among LPS141, LP6, and MESSA cells in a dose-dependent manner. ETC-168 decreased cells of S and G2/M phases, while no significant induction of sub-G1 cells.Inhibition of MNK1/2 by ETC-168 elevated the expression of MNK1/2 at both transcript and protein levels in soft tissue sarcoma (STS) cells.ETC-168 effectively suppressed both p-4E and cell viability in MESSA cells, but not CGP57380 and eFT508.ETC-168 suppresseed phosphorylation of ribosomal protein S6 (RPS6) in sensitive STS cell, decreased expression of E2F1, FOXM1, and WEE1.Inhibition of MCL1 via S63845 synergizes with ETC-168 against STS cells.
Химические свойства
- CAS №
- 1464150-99-9
- Брутто-формула
- C₂₄H₁₉N₅O₂
- Мол. масса
- 409.44 г/моль
- SMILES
- C(#N)C1=CC=C(C2N3C(=NC=2)C=CC(C2=CC=C(C(N4CCOCC4)=O)C=C2)=N3)C=C1
- Синонимы
- Benzonitrile, 4-[6-[4-(4-morpholinylcarbonyl)phenyl]imidazo[1,2-b]pyridazin-3-yl]-
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.