Size : 5mg
Synonyms: AS 605240
| Description | AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50/Ki: 87.8 nM). |
| Targets & IC50 | PI3Kγ:87.8 nM, PI3Kα:60 nM, PI3Kδ:300 nM, PI3Kβ:270 nM |
| In vitro | In the obesity-induced diabetic ob/ob mouse model, AS-605240 at a dosage of 10 mg/kg reduces blood glucose levels, and significantly improves insulin sensitivity and glucose tolerance without affecting body weight, while a higher dosage of 30 mg/kg demonstrates enhanced efficacy with only minor impact on body weight. AS-605240 also reduces the quantity of ATMs and circulating levels of MCP-1. Furthermore, at a dosage of 50 mg/kg, AS-605240 offers protection against symptoms of αCII-induced arthritis and inhibits arthritis inflammation and damage in a collagen-induced arthritis mouse model. Additionally, AS-605240 decreases neutrophil chemotaxis in mice with RANTES-induced peritonitis (ED50: 9.1 mg/kg). |
| In vivo | In bone marrow-derived monocytes, AS-605240 (1 μM) inhibits PKB phosphorylation induced by MCP-1 or CSF-1. In the synapses of the SC-CA1 region in mice, AS-605240 (100 nM) abrogates NMDAR LTD without affecting mGluR LTD and LTP. Furthermore, AS-605240 exhibits inhibition of PI3Kα/β/δ with IC50 values of 60, 270, and 300 nM, respectively. It also inhibits C5a-regulated PKB phosphorylation with an IC50 of 90 nM. |
| Synonyms | AS 605240 |
| Kinase Assay | In vitro PI3K lipid kinase assay: (1) For PI3Kγ: human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 μM ATP/100 nCi γ[33P]ATP, final concentrations) and lipid vesicles containing 18 μM PtdIns and 250 μM of PtdSer (final concentrations), in the presence of AS-605240 or DMSO. Kinase reaction is stopped by adding 250 μg of Neomycin-coated Scintillation Proximity Assay (SPA) beads. (2) For PI3Kα, β, and δ: varying amounts of ATP are incubated with the different purified PI3K isoforms and saturating concentrations of PtdIns. Consequently, IC50 determinations with PI3Kα, β, and δ, to evaluate inhibitor selectivity are performed as follows: 60 ng of PI3Kα are incubated at RT with kinase buffer, as described for PI3Kγ (but containing 89 μM ATP/300 nCi γ[33P]ATP and no Na Cholate, instead) and lipid vesicles containing 212 μM PtdIns and 58 μM of PtdSer. 100 ng of PI3Kβ are incubated at RT with kinase buffer (containing 70 μM ATP/300 nCi γ[33P]ATP, 4 mM MgCl2 and no Na Cholate) and lipid vesicles containing 225 μM PtdIns and 45 μM of PtdSer. 90 ng of PI3Kδ are incubated with kinase buffer (containing 65 μM ATP/300 nCi γ[33P]ATP, 1 mM MgCl2, and no Na Cholate) and lipid vesicles containing 100 μM PtdIns and 170 μM of PtdSer. The reactions are stopped after 2 hours. |
| Cell Research | After a 3-hour starvation in serum-free medium, Cells are pretreated with AS-605240 or DMSO for 30 min and stimulated for 5 min with 50 nM of C5a. PKB phosphorylation is monitored using phosphorylated Ser473 Akt-specific antibody and standard ELISA protocols. (Only for Reference) |
| Molecular Weight | 257.27 |
| Formula | C12H7N3O2S |
| Cas No. | 648450-29-7 |
| Smiles | C(C1=CC2=C(C=C1)N=CC=N2)=C3C(=O)NC(=O)S3 |
| Relative Density. | 1.553g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | DMSO: 1 mg/mL (3.89 mM), Sonication is recommended.  | ||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 0.23 mg/mL (0.89 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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