Table 1.

PKI-402 IC50 values in human tumor cell line growth inhibition assays

Cell lineMutationsIC50 (μmol/L)SD (n ≥ 3)
Breast
    MDA-MB-361PIK3CA0.0060.001
    MDA-MB-468PTEN, RB, p530.0090.001
    T47Dp53, PIK3CA0.0130.002
    BT474PIK3CA, p530.0260.006
    MCF7PIK3CA0.1010.014
Colon
    HCT116K-Ras, PIK3CA0.0330.002
    HT29B-Raf, PIK3CA, p530.1360.041
    DLD1K-Ras, PIK3CA0.2270.009
Lung (NSCLC)
    NCI-H157K-Ras, STK11, p530.0360.004
    NCI-H460K-Ras, PIK3CA, STK110.0890.003
    A549K-Ras, STK110.1160.031
    NCI-H2170p530.1270.027
    NCI-H1975EGFR, PIK3CA, p530.2100.015
    NCI-H1650EGFR, p530.3490.061
Pancreas
    MIA-PaCa-2K-Ras, p530.0510.003
Brain (glioma)
    U87MGPTEN0.0770.017
Prostate
    PC3PTEN, p530.0160.002
Epidermoid
    KB0.0270.003
Renal
    A498VHL0.2680.002
    786-0PTEN, VHL, p530.3340.060