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. 2023 Nov 15;66(23):15629–15647. doi: 10.1021/acs.jmedchem.3c01233

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
a

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.

b

Cell proliferation was measured by the fluorescence intensity of an incorporated nuclear dye.

c

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.

d

Cell cycle arrest was measured by labeling of mitotic cells with a fluorescently labeled antibody to phosphorylated histone H3.