Duvelisib R enantiomer

• CAT Number: I001051
• CAS Number: 1261590-48-0
• Molecular Formula: C22H17ClN6O
• Molecular Weight: 416.86
• Purity: ≥95%
• Target: PI3K
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder

Duvelisib (R enantiomer) is a novel and selective PI3K δ/γ inhibitor with 2.5 nM / 27 nM (PI3K δ/γ), highly selective for PI3K δ/γ than other protein kinases.Target: PI3K δ/γin vitro: Human peripheral blood CD19+ B cells were stimulated with anti-IgM and anti-CD40 antibodies in the presence or absence of IPI-145 for 96 hr. IPI-145 inhibited human B cell proliferation with an average IC50 value of 0.5 nM[1]in vivo: Beginning at this time, animals were orally dosed daily for 20 weeks with vehicle, IPI-145 (1, 5, or 10 mg/kg), or a dexamethasone control (2 mg/kg). Proteinuria was significantly reduced at study termination for all IPI-145-treated mice compared with vehicle animals, as well as in the dexamethasone control group [1].

Reference

[1]. David G. Winkler, Kerrie L. Faia et,al. PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Responses and Suppresses Activity in Autoimmune and Inflammatory Disease Models. Chemistry & Biology.2013 Nov 21, Pages 1364-1374
[2]. K Balakrishnan, M Peluso et al. The Phosphoinositide-3-Kinase (PI3K)-Delta and Gamma Inhibitor, IPI-145, Overcomes Signals from the PI3K/AKT/S6 Pathway and Promotes Apoptosis in CLL. Leukemia. 2015 Sep; 29(9): 1811–1822.