Leniolisib phosphate

• CAT Number: I030635
• CAS Number: 1354691-97-6
• Molecular Formula: C21H28F3N6O6P
• Molecular Weight: 548.45
• Purity: 98%
• Synonyms: 1-[(3S)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one;phosphoric acid
• Target: PI3Kδ
• Target Protein: O00329
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: hPDE4D (IC50 = 4.7 μM) and 5HT2B (IC50 = 7.7 μM)
• InChI: InChI=1S/C21H25F3N6O2.H3O4P/c1-3-18(31)30-6-4-13(10-30)28-19-15-11-29(7-5-17(15)26-12-27-19)14-8-16(21(22,23)24)20(32-2)25-9-14;1-5(2,3)4/h8-9,12-13H,3-7,10-11H2,1-2H3,(H,26,27,28);(H3,1,2,3,4)/t13-;/m0./s1
• InChIKey: XXEDEGOAYSGNPS-ZOWNYOTGSA-N
• SMILES: CCC(=O)N1CC[C@@H](C1)NC2=NC=NC3=C2CN(CC3)C4=CC(=C(N=C4)OC)C(F)(F)F.OP(=O)(O)O

Leniolisib phosphate（Cat No.:I030635）is a potent, selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), an enzyme involved in the regulation of immune cell function. It is being investigated for the treatment of activated PI3K delta syndrome (APDS), a rare primary immunodeficiency disorder. By inhibiting PI3Kδ, Leniolisib phosphate reduces the overactivation of immune cells, helping to restore immune balance and alleviate symptoms associated with APDS. Its targeted mechanism offers a promising therapeutic option for patients with this genetic disorder, improving immune function and overall health outcomes.

Reference

[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
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[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.
[Content Brief]