All AbMole products are for research use only, cannot be used for human consumption.
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
BioRxiv. 2021 Jan 20;427305.
Targeted delivery of a phosphoinositide 3-kinase γ inhibitor to restore organ function in sepsis through dye-functionalized lipid nanocarriers
AS605240 purchased from AbMole
 |
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 |
|---|
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
| Apitolisib (GDC-0980)
Apitolisib (GDC-0980; GNE 390; RG 7422) is a potent, highly selective, oral, dual inhibitor of class I PI3K and mTOR. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
