853910-61-9

生物活性

Orally potent and selective dual PI3K/mTOR inhibitor; IC50 values to be 72, 2336, 201 and 382 nM for PI3K p110 alpha, beta, delta and gamma isoforms, respectively; inhibition of PI3K/mTOR pathway like NVP-BEZ235, BBD130 efficiently attenuates growth and proliferation of melanoma primary tumors and metastasis.

参考文献

R Marone et al. Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors. Mol. Cancer Res. 2009, 7(4), 601-613. [online] F Stauffer et al. Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway. Bioorg. Med. Chem. Lett. 2008, 18, 1027-1030. SM Maria, P Furet and F Stauffer. Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway. Future Med. Chem. 2009, 1(1), 137-155