AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. AS-605240 inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively. AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg.
EMBO Mol Med. 2021 Oct 7;13(10):e14436.
Targeted delivery of a phosphoinositide 3-kinase γ inhibitor to restore organ function in sepsis
AS605240 purchased from AbMole
Cell Experiment | |
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Cell lines | Jurkat cells |
Preparation method | Cell lines culture and survival assays. Cell lines were cultured in RPMI-1640 medium, 10% fetal bovine serum (FBS), and penicillin/streptomycin at 37°C and 5% CO2. Medium was changed 12–24 h before all experiments. To measure IC50 values, cells (2–6 × 104) were incubated for 96 h with increasing concentrations of AS605240, prednisolone, L-asparaginase, MTX or DNR. To measure Combination Index (CI) values between AS605240 and the other drugs, 2-fold ratios of the calculated IC50 values (0.25×, 0.5×, 1×, 2× or 4×) of each drug were used either in combination or as single drugs. Cells were treated for a total of 96 h. When drug scheduling was applied, one of the drugs was added 48 h after the start of the experiment. Cell viability was measured by the MTT assay. IC50 and CI values were calculated with the GraphPad Prism 5 (GraphPad Software, La Jolla, CA, USA) and Calcusyn (Biosoft, Cambridge, UK) [65] softwares, respectively. |
Concentrations | 0.1~100 μM |
Incubation time | 24 h |
Animal Experiment | |
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Animal models | mouse CIA |
Formulation | 0.5% carboxymethylcellulose /0.25% Tween- 20 (Sigma) |
Dosages | 50mg/kg twice a day for 7 days |
Administration | orally |
Molecular Weight | 257.27 |
Formula | C12H7N3O2S |
CAS Number | 648450-29-7 |
Solubility (25°C) | DMSO 4 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.
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