| AS-605240Potent and selective PI 3-Kγ inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 99.45%
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Chemical structure
| Description | AS-605240 is a selective inhibitor of PI3Kγ with an IC50 value of 8 nM. | |||||
| Targets | PI3Kγ | PI3Kα | PI3Kβ | PI3Kδ | ||
| IC50 | 8 nM | 60 nM | 270 nM | 300 nM | ||
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| Cas No. | 648450-29-7 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | C1=CC2=NC=CN=C2C=C1C=C3C(=O)NC(=O)S3 | ||
| Formula | C12H7N3O2S | M.Wt | 257.27 |
| Solubility | ≥4.28mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AS-605240 is a selective PI3K γ inhibitor with an IC50 of 8 nM. [1]
PI3Ks are a family of enzymes, which phosphorylate the 3’- OH position of the inositol ring of phosphoinositides.They have been divided into three classes on the basis of structural features and in vitro lipid substrate specificity. The three class-Ia PI3-kinases (p110 α / β / δ ) and the sole class-Ib PI 3-kinase (p110 γ ) couple growth factor receptors and G-protein-coupled receptors, respectively, to a wide range of downstream pathways. Signal transduction via the PI3K/Akt pathway is essential for regulating cellular responses, including proliferation, survival, migration, motility and tumorigenesis, in a variety of cell types. The key selectivity features were identified by co-crystallization with PI3Kγ, which revealed that thiazolidinedione nitrogen makes a salt – bridge interaction with the side chain of Lys-833, and also forms the link to Val-882.[1,2]
AS-605240 is a cell permeable inhibitor for PI3Ks and inhibits p110 α/β/γ/δ in vitro?with IC50 values of 0.06, 0.27, 0.008 0.3 μΜ, respectively. AS-605240 was tested its ability to inhibit C5a-mediated PKB phosphorylation in RAW264 mouse macrophages and AS-605240 showed an IC50 of 0.09 mM. [1]
As in many in?ammatory processes, neutrophils are predominant in the initial in?ux of leukocytes, followed by monocytes-macrophages and lymphocytes. in vivo efficacy in blocking leukocyte migration assays were conducted, AS-605240 was tested in two different mouse models of peritonitis, including RANTES-induced or thioglycollate, the outcome showed ED50 of 9.1 mg/kg and 10 mg/kg respectively. AS-605240 also show that it is an orally active, selective PI3Kγ inhibitor suppresses joint inflammation and damage in a mouse model of collagen-induced arthritis.[1]
References:[1]. Camps M, Rückle T, Ji H, et al. Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis[J]. Nature medicine, 2005, 11(9): 936-943.[2]. Marone R, Cmiljanovic V, Giese B, et al. Targeting phosphoinositide 3-kinase—moving towards therapy[J]. Biochimica et Biophysica Acta (BBA)-Proteins and Proteomics, 2008, 1784(1): 159-185.
