ATM Inhibitor-1

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC₅₀ of 0.7 nM, 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). ATM Inhibitor-1 exhibits anti-tumor activity^[1]. IC50 & Target: IC50: 0.7 nM (ATM), 21 μM (mTOR), 2.8 μM (DNAPK), 3.8 μM (PI3Kα), 10.3 μM (PI3Kβ), 3 μM (PI3Kγ), 0.73 μM (PI3Kδ)^[1] In Vitro: ATM Inhibitor-1 (Compound 21) is a highly potent, selective and orally active ATM Inhibitor, with an IC₅₀ of 0.7 nM, 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)^[1].
In cellular assays, ATM Inhibitor-1 exhibits IC₅₀s of 2.8 nM, >30 μM and >19 μM for ATM, ATR/PI3Kα and PI3Kβ/mTOR, respectively^[1]. In Vivo: ATM Inhibitor-1 (Compound 21; 50 mg/kg p.o. once daily for 3 days every week starting 24 h post-irinotecan dosing, 21 days) in combination with 50 mg/kg irinotecan significantly reduces tumor growth in SW620 mice model^[1].