Биологическая активность
M3541 (M 3541) is a novel мощный, селективный and ATP-competitive ATM киназы ингибитор с IC50 of 0.25 nM (ATP, 10 uM).M3541 displays a good margin of selectivity (>60-fold) against the closely related PIKK family members with DNA-PK, PI3K isoforms, mTOR, and ATR.M3541 inhibits the phosphorylation of ATM as well as its клеточный substrates CHK2, KAP1, and p53 in a concentration-dependent manner in A549 cells.M3541 inhibits double strand break repair and sensitizes cancer cells to radiation.M3541 suppresses ATM pathway activity and potentiates radiation efficacy in xenograft models of human cancer, synergizes with topoisomerase and PARP inhibitors.
Оригинал на английском
M3541 (M 3541) is a novel potent, selective and ATP-competitive ATM kinase inhibitor with IC50 of 0.25 nM (ATP, 10 uM).M3541 displays a good margin of selectivity (>60-fold) against the closely related PIKK family members with DNA-PK, PI3K isoforms, mTOR, and ATR.M3541 inhibits the phosphorylation of ATM as well as its cellular substrates CHK2, KAP1, and p53 in a concentration-dependent manner in A549 cells.M3541 inhibits double strand break repair and sensitizes cancer cells to radiation.M3541 suppresses ATM pathway activity and potentiates radiation efficacy in xenograft models of human cancer, synergizes with topoisomerase and PARP inhibitors.
Химические свойства
- CAS №
- 1360628-91-6
- Брутто-формула
- C₂₃H₁₇FN₆O₂
- Мол. масса
- 428.42 г/моль
- SMILES
- C(#N)C1=CC=C(N2C3C4C(N=CC=3N(C)C2=O)=CC(OC)=C(C2=CN(C)N=C2)C=4)C(F)=C1
- Синонимы
- Benzonitrile, 4-[2,3-dihydro-7-methoxy-3-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-oxo-1H-imidazo[4,5-c]quinolin-1-yl]-3-fluoro-; 4-[2,3-Dihydro-7-methoxy-3-methyl-8-(1-methyl-1H-pyrazol-4-yl)-2-oxo-1H-imidazo[4,5-c]quinolin-1-yl]-3-fluorobenzonitrile; M3541
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.