Table 5. Summary of Compound 28’s Activity in TNBC Cell Linesa.
Cell countb |
Apoptosisc |
||||
---|---|---|---|---|---|
Cell line | GI50(μM) | IC50(μM) | 5-Fold Induction (μM) | Emax | dG1/S cell cycle block (μM) |
BT-20 | 0.60 | 0.97 | 7.73 | 6.22 | 0.95 |
BT-549 | 0.80 | 0.94 | 0.74 | 7.99 | 1.42 |
MDA-MB-231 | 0.80 | 0.88 | 0.64 | 32.4 | 1.78 |
MT-3 | 0.53 | 0.60 | 0.67 | 15.1 | 1.16 |
Hs 578T | 1.06 | 1.23 | 0.78 | 7.24 | 2.13 |
BT-20, BT-549, MDA-MB-231, MT-3, and Hs 578T were treated with compound 28 in a serial dilution over 10 concentrations with a maximum of 0.1% DMSO over 72 h.
Cell proliferation was measured by the fluorescence intensity of an incorporated nuclear dye.
Apoptosis was measured by the fluorescence intensity of a fluorescently labeled antibody to activated caspase 3. The output is shown as a fold increase of apoptotic signal over vehicle background normalized to the relative cell count in each well. The concentration of test compound that caused a 5-fold induction in the caspase-3 signal is reported, indicating a significant apoptosis induction.
Cell cycle arrest was measured by labeling of mitotic cells with a fluorescently labeled antibody to phosphorylated histone H3.