A potent PI3K inhibitor
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GSK1059615

Item No. 11569

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5Z-[[4-(4-pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidinedione
CAS Number
958852-01-2
Molecular Formula
C18H11N3O2S
Formula Weight
333.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2.5 mg/mlDMSO: 3 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
295, 347 nm
SMILES
O=C(NC/1=O)SC1=C/C2=CC(C(C3=CC=NC=C3)=CC=N4)=C4C=C2
InChi Code
InChI=1S/C18H11N3O2S/c22-17-16(24-18(23)21-17)10-11-1-2-15-14(9-11)13(5-8-20-15)12-3-6-19-7-4-12/h1-10H,(H,21,22,23)/b16-10-
InChi Key
QDITZBLZQQZVEE-YBEGLDIGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $123

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    25 mg

    $278

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    50 mg

    $502

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    Product Description

    PI 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation. Its signaling pathway is the most commonly mutated pathway in human cancers. GSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM) and the common activating mutants of p110α (E542K, E545K, and H1047R) found in cancer.1,2 It prevents proliferation in BT474 tumor xenografts and reduces MAPK signaling following twice daily dosing at 25 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Knight, S.D., Adams, N.D., Burgess, J.L., et al. Discovery of GSK2126458, a highly potent inhibitor of P13K and the mammalian target of rapamycin. ACS Med. Chem. Lett. 1(1), 39-43 (2010).

    2. Aziz, S.A., Davies, M., Pick, E., et al. Phosphatidylinositol-3-kinase as a therapeutic target in melanoma. Clin. Cancer Res. 15(9), 3029-3036 (2009).