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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
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Source | Oncotarget (2015). Figure 3. AS605240 |
| Method | cell apoptosis assay | |
| Cell Lines | T-ALL cells | |
| Concentrations | 10 μM | |
| Incubation Time | 8 h | |
| Results | AS605240 inhibited p-Akt (Figure 3a–3b) and PIP3 (Figure 3c) accumulation and promoted apoptosis in both T-ALL cell lines and primary cells, with activation of Caspase-3 (Figure 3d, Supplementary Figure 5). |
| Cell Experiment | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related PI3K Products |
|---|
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PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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