A potent inhibitor of PI3Kγ
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Alternative(s)
10007707AS-605240
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AS-605240 (potassium salt)

Item No. 9000980

Technical Information
Formal Name
5-(6-quinoxalinylmethylene)-2,4-thiazolidinedione, monopotassium salt
Molecular Formula
C12H6N3O2S • K
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
λmax
251, 291, 370 nm
SMILES
O=C(S/1)[N-]C(C1=C\C2=CC3=C(C=C2)N=CC=N3)=O.[K+]
InChi Code
InChI=1S/C12H7N3O2S.K/c16-11-10(18-12(17)15-11)6-7-1-2-8-9(5-7)14-4-3-13-8;/h1-6H,(H,15,16,17);/q;+1/p-1/b10-6-;
InChi Key
OVISXPIEMMRFGY-OTUCAILMSA-M
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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    Product Description

    AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis.1 It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.1 AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg. AS-605240 (potassium salt) has improved solubility compared to AS-605240 (Item No. 10007707).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Camps, M., Rückle, T., Ji, H., et alBlockade of PI3K g suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat. Med. 11(9), 936-943 (2005).