AS 605240

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Cat.No. 3578 - AS 605240 | C12H7N3O2S | CAS No. 648450-29-7
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)
Datasheet
Citations (2)
Literature

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 0.26 1mM 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.89 mL 19.43 mL 38.87 mL
5 mM 0.78 mL 3.89 mL 7.77 mL
10 mM 0.39 mL 1.94 mL 3.89 mL
50 mM 0.08 mL 0.39 mL 0.78 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:

Wang et al (2009) Phosphoinositide 3-kinase γ inhibitor ameliorates concanavalin A-induced hepatic injury in mice. Biochem.Biophys.Res.Comm. 386 569 PMID:


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View all PI 3-kinase Inhibitors

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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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