Leniolisib phosphate

Leniolisib (CDZ173) phosphate is a potent and selective PI3Kδ inhibitor. Leniolisib phosphate has the potential for immunodeficiency disorders treatment.

PI3Kδ: 11 nM (IC₅₀); PI3Kα: 280 nM (IC₅₀); PI3Kβ: 480 nM (IC₅₀); PI3Kγ: 2.57 nM (IC₅₀); DNA-PK: 880 nM (IC₅₀)

[1] Rao V, et al. Effective 'Activated PI3Kd Syndrome' -targeted therapy with PI3Kd inhibitor leniolisib. The New England journal of medicine: NEJM. ISSN 0028-4793; 1533-4406 DOI:10.1182/blood-2017-08-801191
[2] Hoegenauer K, et al. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. DOI:10.1021/acsmedchemlett.7b00293