Description
XL 147 can inhibit p110-alpha with IC50 of 40 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C21H16N6O2S2
Chemical Name
N-(3-(benzo[c][1,2,5]thiadiazol-5-ylamino)quinoxalin-2-yl)-4-methylbenzenesulfonamide
Solubility
DMSO 89 mg/mL Water
In vitro
XL147, an ATP-competitive reversible PI3K inhibitor, exhibits an IC50 against WT and mutant p110 alpha of approximately 40 nM. Treatment with XL147 can inhibit the monolayer growth of all cell lines in a dose-dependent manner. The IC50 value is around 6 uM. At 20 uM, XL147 induced cell death as revealed by the reduction. In all cell lines, treatment with XL147 resulted in dose-dependent inhibition of PI3K as measured by pAKT(S473). Consistent with the inhibition of cell proliferation, XL147 induced a reduction in cyclin D1 and pRB and an increase in levels of the CDK inhibitor p27(KIP1).
In vivo
Addition of trastuzumab or lapatinib would enhance the antitumor effect of XL147 against HER2-dependent xenografts.
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