Table 1.
Antiproliferative activity of DFP and DFP-based PROTACs.
| Compound | Cell Line and IC50 Value (µM) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| A549 | DU-145 | LNCaP | HepG2 | SK-HEP-1 | MCF-7 | MDA-MB-231 | MDA-MB-453 | Vero | |
| DFP | 111.9a | 134.1a | 85.9a | ||||||
| DW-229 | 7.69 | 1.21 ± 0.3 | 2.58 ± 0.7 | 4.17 ± 0.7 | 1.09 | <0.5b | 8.87 ± 2.1b | 3.86 ± 0.4b | 23.81 ± 4.1b |
| DW-451 | 14.32 | 3.46 ± 0.1 | 3.82 ± 0.4 | 10.72 ± 0.7 | 1.26 | 7.28 ± 1.90 | 5.54 ± 0.8 | 7.79 ± 1.6 | 56.64 ± 2.9 |
| DW-449 | 1.96 | <0.5 | 0.54 ± 0.0 | 0.54 ± 0.1 | <0.5 | 3.21 ± 0.6b | 1.15 ± 0.3b | 1.85 ± 0.2b | 13.93 ± 0.3 |
| DW-455 | 8.10 ± 2.0 | <0.5 | 0.97 ± 0.1 | 2.51 ± 1.2 | <0.5 | 3.79 ± 0.5 | 2.93 ± 0.9 | 3.87 ± 1.1 | 16.75 ± 2.9 |
a
Khodaverdian et al., 2019
b
p < 0.0001 in comparison to Vero cell line