产品描述:
XL147 is an inhibitor of class I PI3Ks (IC50s = 0.039, 0.036, 0.023, and 0.383 µM for p110α, -δ, -γ, and -β, respectively).{65046} It is selective for class I PI3Ks over the class III PI3K vacuolar protein sorting 34 (Vps34; IC50 = 6.974 µM), as well as DNA protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) (IC50s = 4.75 and >15 µM, respectively). XL147 inhibits the proliferation of MCF-7 breast and PC3 prostate cancer cells (IC50s = 9.669 and 16.492 µM, respectively). It reduces tumor growth in a BT474 breast cancer mouse xenograft model when administered alone or in combination with trastuzumab or lapatinib (Item No. 11493).{29153}