533435 Sigma-AldrichPI 3-Kδ Inhibitor, PI-3065 - CAS 955977-50-1 - Calbiochem

This product has been discontinued.

A cell permeable, bioavailable thienopyrinidine derived compound that acts as a highly potent and selective inhibitor of PI 3-kinase δ (p110δ; K_i = 1.5 nM, IC₅₀ = 15 nM). Exhibits >100-fold selectivity over p100α, p100β, and p100γ isoforms (K_i = 110, 130, and 940 nM, respectively) and does not affect the activity of DNA-PK and mTOR (IC₅₀ is >10 µM and >9 µM, respectively). Shown to suppress 4T1 breast tumor growth and macroscopic metastasis in mice and prolongs their survival rate. Displays favorable pharmacokinetic properties with t_1/2 = 1 h, C_max = 6.88 µM, and AUC = 42 µM/h (75 mg/kg, p.o in BALB/c mice).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.