A pan class I PI3K inhibitor
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ZSTK474

Item No. 17381

Technical Information
Formal Name
2-(difluoromethyl)-1-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-1H-benzimidazole
CAS Number
475110-96-4
Molecular Formula
C19H21F2N7O2
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 25 mg/mlDMSO: 20 mg/ml
λmax
240 nm
SMILES
FC(F)C1=NC(C=CC=C2)=C2N1C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3
InChi Code
InChI=1S/C19H21F2N7O2/c20-15(21)16-22-13-3-1-2-4-14(13)28(16)19-24-17(26-5-9-29-10-6-26)23-18(25-19)27-7-11-30-12-8-27/h1-4,15H,5-12H2
InChi Key
HGVNLRPZOWWDKD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ZSTK474 is a triazine derivative that acts as an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (IC50s = 17, 53, and 6 nM for p110β, -γ, and -δ, respectively).1 It is selective for PI3K, as it has negligible activity against 139 other kinases when tested at 30 µM.1 ZSTK474 is orally bioavailable and shows strong antitumor activity against human cancer xenografts in mice.1 The efficacy of ZSTK474 against certain cancer cells and tumors can be enhanced by combination therapy.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yaguchi, S.i., Fukui, Y., Koshimizu, I., et alAntitumor activity of ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor. J. Natl. Cancer Inst. 98(8), 545-556 (2006).

    2. Lin, L., Gaut, D., Hu, K., et alDual targeting of glioblastoma multiforme with a proteasome inhibitor (Velcade) and a phosphatidylinositol 3-kinase inhibitor (ZSTK474). Int. J. Oncol. 44, 557-562 (2014).

    3. Bertazza, L., Barollo, S., Radu, C.M., et alSynergistic antitumour activity of RAF265 and ZSTK474 on human TT medullary thyroid cancer cells. J. Cell. Mol. Med. 19(9), 2244-2252 (2015).