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Duvelisib (IPI-145) is a novel and selective PI3K δ/γ inhibitor with IC50 of 23 pM and 243 pM, respectively. IPI-145 prevents the activation of the PI3K delta/gamma-mediated signaling pathways which may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. Duvelisib (IPI-145) suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM. IPI-145 was well tolerated and clinically active in a broad range of malignancies, including iNHL. IPI-145 (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model.
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Source | Blood (2014). Figure 1. IPI-145 |
| Method | immunoblotting | |
| Cell Lines | CLL cells | |
| Concentrations | 0.01 to 1 μM | |
| Incubation Time | 24 h | |
| Results | Cell viability was measured every 24 hours; 0.25 to 5 μM IPI-145 exhibited concentration and timedependent induction of cytotoxicity in CLL. |
| Molecular Weight | 416.86 |
| Formula | C22H17ClN6O |
| CAS Number | 1201438-56-3 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Anna Maria Frustaci, et al. Duvelisib for the treatment of chronic lymphocytic leukemia
[2] No authors listed. Duvelisib
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