Selective inhibitor of PI3Kγ
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AS-041164

Item No. 13622

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-(1,3-benzodioxol-5-ylmethylene)-2,4-thiazolidinedione
CAS Number
6318-41-8
Molecular Formula
C11H7NO4S
Formula Weight
249.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:9): 0.1 mg/mlDMSO: 25 mg/ml
λmax
355 nm
SMILES
O=C(/C(S1)=C/C2=CC=C3C(OCO3)=C2)NC1=O
InChi Code
InChI=1S/C11H7NO4S/c13-10-9(17-11(14)12-10)4-6-1-2-7-8(3-6)16-5-15-7/h1-4H,5H2,(H,12,13,14)/b9-4-
InChi Key
SDGWAUUPHUBJNQ-WTKPLQERSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $80

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    10 mg

    $102

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    25 mg

    $228

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    50 mg

    $381

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    Product Description

    The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.1 AS-041164 is a potent inhibitor of PI3K 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).2 When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.2 When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hirsch, E., Ciraolo, E., Ghigo, A., et al. Taming the PI3K team to hold inflammation and cancer at bay. Pharmacol. Ther. 118(2), 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. J. Pharmacol. Exp. Ther. 322(3), 923-930 (2007).