AS 041164CAS: 1146702-72-8
MF: C11H7NO4S
MW: 249.2
A potent inhibitor of PI 3-kinase.

AS 041164 (CAS 1146702-72-8)

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Synonym: 5-(1,3-benzodioxol-5-ylmethylene)-2,4-thiazolidinedione
Application: A potent inhibitor of PI 3-kinase
CAS Number: 1146702-72-8
Molecular Weight: 249.2
Molecular Formula: C11H7NO4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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AS 041164 is a potent inhibitor of PI 3-kinase with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM). When tested at 1.0 μM, it shows little or no activity against 38 other common kinases. When given orally to mice, AS 041164 shows a pharmacokinetic profile that is similar to the general PI 3-kinase inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS 041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.


References

1 Hirsch, E., Ciraolo, E., Ghigo, A., et al. Taming the PI3K team to hold inflammation and cancer at bay. Pharmacology & Therapeutics 118 192-205 (2008). 2 Ferrandi, C., Ardissone, V., Ferro, P., et al. Phosphoinositide 3-kinase γ inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. JPET 322 923-930 (2007).

Physical State :
Solid
Solubility :
Soluble in DMSO (~25 mg/ml), dimethyl formamide (~25 mg/ml), and 1:9 ethanol:PBS(pH 7.2) (~0.1 mg/ml).
Storage :
Store at -20° C
Melting Point :
224.44° C
Boiling Point :
525.36° C
Density :
1.60 g/cm3
Refractive Index :
n20D 1.73
IC50 :
PI3Kγ : IC50 = 70 nM; PI3Kα: IC50 = 240 nM; PI3Kβ: IC50 = 1.45 µM; PI3Kδ: IC50 = 1.70 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
1269519
SMILES :
C1OC2=C(O1)C=C(C=C2)/C=C\\3/C(=O)NC(=O)S3

Download SDS (MSDS)

Certificate of Analysis

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