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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

492.61

C₂₇H₃₆N₆O₃

2135639-94-8

C[C@@H](C1CCOCC1)NC2=C(C(NC)=O)N=NC3=CC=C(C4=CC=C(OCCCN(C)C)N=C4)C=C32

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Barlaam B, et al. Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. CS Med Chem Lett. 2018 Jul 13;9(8):809-814.  [Content Brief]