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ZSTK-474

Chemical Structure : ZSTK-474

CAS No.: 475110-96-4

ZSTK-474 (ZSTK474;ZSTK 474)

Catalog No.: PC-45869Not For Human Use, Lab Use Only.

ZSTK-474 (ZSTK474) is a potent inhibitor of class I PI3K isoforms with IC50 of 17 nM, 53 nM, and 6 nM for p110β, p110γ, and p110δ, respectively.

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Biological Activity

ZSTK-474 (ZSTK474) is a potent inhibitor of class I PI3K isoforms with IC50 of 17 nM, 53 nM, and 6 nM for p110β, p110γ, and p110δ, respectively.
ZSTK-474 (ZSTK474) shows potent antiproliferative activity against a panel of 39 human cancer cell lines with mean GI50 of 0.32 uM.
ZSTK-474 (ZSTK474) is more effectively than that of LY294002 or wortmannin.
ZSTK-474 (ZSTK474) induces apoptosis in OVCAR3 cells, and induces complete G1-phase arrest but not apoptosis in A549 cells at 10 uM.
ZSTK-474 (ZSTK474) completely inhibits the growth of A549, PC-3, and WiDr xenografts in mice at 400mg/kg; and induces the regression of A549 xenograft tumors.

Physicochemical Properties

M.Wt 417.4125
Formula C19H21F2N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Benzimidazole, 2-(difluoromethyl)-1-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-

References

1. Yaguchi S, et al. J Natl Cancer Inst, 2006, 98(8), 545-556.

2. Kong D, et al. Cancer Sci, 2007, 98(10), 1638-1642.

3. Kong D, et al. Eur J Cancer, 2009, 45(5), 857-865.

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