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Submit ReviewAS 605240
Description: Potent and selective PI 3-kinase γ (PI 3-Kγ) inhibitor
Chemical Name: 5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione
Purity: ≥98% (HPLC)
Biological Activity
Potent and selective inhibitor of PI 3-kinase γ (PI 3-Kγ) (IC50 = 8 nM). Displays 30-fold selectivity over PI 3-Kδ and PI 3-Kβ and 7.5-fold selectivity over PI 3-Kα. Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis. Orally active and ATP-competitive.
Technical Data
| M. Wt | 257.27 |
| Formula | C12H7N3O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 648450-29-7 |
| PubChem ID | 5289247 |
| InChI Key | SQWZFLMPDUSYGV-POHAHGRESA-N |
| Smiles | O=C(/C(S3)=C/C(C=C2)=CC1=C2N=CC=N1)NC3=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 0.26 | 1 with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 257.27. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.01 mM | 388.7 mL | 1943.48 mL | 3886.97 mL |
| 0.05 mM | 77.74 mL | 388.7 mL | 777.39 mL |
| 0.1 mM | 38.87 mL | 194.35 mL | 388.7 mL |
| 0.5 mM | 7.77 mL | 38.87 mL | 77.74 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Peng et al (2010) Inhibition of phosphoinositide 3-kinase ameliorates dextran sodium sulfate-induced colitis in mice. J.Pharmacol.Exp.Ther. 332 46 PMID: 19828878
Camps et al (2005) Blockade of PI3Kγ suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nature Med. 11 936
Wang et al (2009) Phosphoinositide 3-kinase γ inhibitor ameliorates concanavalin A-induced hepatic injury in mice. Biochem.Biophys.Res.Comm. 386 569
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Keywords: AS 605240, AS 605240 supplier, AS605240, PI3Kgamma, PI3Kγ, PI, 3-kinasegamma, 3-kinaseg, 3-kinaseγ, phosphoinositide, 3, kinases, gamma, γ, Potent, selective, inhibitors, inhibits, inositol, lipids, signalling, signaling, orally, active, ATP-competitive, 3-Kinase, Inositol, Lipids, 3578, Tocris Bioscience
2 Citations for AS 605240
Citations are publications that use Tocris products. Selected citations for AS 605240 include:
Beauséjour et al (2012) Integrin/Fak/Src-mediated regulation of cell survival and anoikis in human intestinal epithelial crypt cells: selective engagement and roles of PI3-K isoform complexes. Apoptosis 17 566 PMID: 22402981
Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832 PMID: 22434859
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