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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Anna Maria Frustaci, et al. Duvelisib for the treatment of chronic lymphocytic leukemia
[2] No authors listed. Duvelisib
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