atm inhibitor1

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibito (IC50: 0.7 nM) anti-tumor activity. It shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM).

ATMInhibitor-11 (Compound 1) 是一种针对ATM的高效抑制剂，具有0.32 nM的IC50值，并对KAP1磷酸化显示出0.97 nM的IC50抑制效果。此化合物在ICR小鼠的大脑、心脏和血浆中展示了良好的药物暴露性。在NCI-H441异种移植小鼠模型试验中，ATMInhibitor-11展现了显著的抗肿瘤活性。