AZD1390

Description: AZD1390 (AZD-1390) is a novel, potent, selective, first-in-class orally bioavailable and CNS penetrant inhibitor of Ataxia-telangiectasia mutated (ATM) kinase with potential anticancer activity. It has an IC50 of 0.78 nM for inhibiting ATM in cell assays, and is > 10, 000-fold more selective over closely related PIKK family of enzymes and excellent selectivity across a broad range of kinases. AZD1390 is able to cross the blood-brain barrier (BBB) which makes it suitable for the treatment of intracranial malignancies. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 is now in early clinical development for use as a radiosensitizer in central nervous system malignancies.

References: Science Advances. 2018, 4(6): eaat1719.