XL-418 

XL-418 is an orally active dual Akt and p70S6K inhibitor with IC₅₀s of 1 nM for Akt1 and 2 nM for p70S6K. XL-418 inhibits the phosphorylation of ribosomal protein S6 and GSK3β. XL-418 can be used for the study of prostate carcinoma and breast cancer^[1].

XL-418 inhibits the phosphorylation of ribosomal protein S6 with IC₅₀ values of 30 nM and 55 nM in A549 and PC-3 cells. XL-418 inhibits the phosphorylation of GSK3β with an IC₅₀ value of 194 nM in PC-3 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

XL-418 (compound 11b; 100 mg/kg; p.o.;twice a day; total five doses) inhibits the phosphorylation of ribosomal protein S6 and GSK3β in the PC-3 prostate carcinoma model^[1].
XL-418 (50 mg/kg; p.o.; once a day; for 15 days) inhibits tumor growth in the PC-3 prostate carcinoma model^[1].
XL-418 (50-100 mg/kg; p.o.; two days every 4 days) shows highly active in this study with 71% tumor growth inhibition for the 50 mg/kg dose and 96% tumor growth inhibition (TGI) for the 100 mg/kg alternate dosing schedule as a single agent^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

609.48

C₂₆H₃₂BrF₃N₈O

871343-09-8

O=C(C1=CC(NCCN2CCCC2)=C(C)C(N3CCN(C4=C5C(NN=C5Br)=NC=N4)CC3)=C1)CCC(F)(F)F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Rice KD, et al. Pyrazolopyrimidines as dual Akt/p70S6K inhibitors. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2693-7.