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AS605240

Cat. No. M1651
AS605240 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 35  USD35 In stock
5mg USD 37  USD37 In stock
10mg USD 57  USD57 In stock
50mg USD 210  USD210 In stock
100mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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).
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Silveira AB, et al. Oncotarget. PI3K inhibition synergizes with glucocorticoids but antagonizes with methotrexate in T-cell acute lymphoblastic leukemia.

[2] Azzi et al. Diabetes. The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes.

[3] Mielcke et al. Eur J Med Chem. Activity of novel quinoxaline-derived chalcones on in vitro glioma cell proliferation.

[4] Kim et al. J Clin Immunol. PI3K-γ inhibition ameliorates acute lung injury through regulation of IκBα/NF-κB pathway and innate immune responses.

[5] Anzinger et al. J Lipid Res. Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL.

[6] Camps M, et al. Nat Med. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.

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