Table 2. IC50 values (nM) of LB-1–LB-12 against CDK9 and IC50 values (μM) of LB-1–LB-12 and AZD5438 against HCT116, RKO and HT-29 cell lines.
| |||||
|---|---|---|---|---|---|
| Compound | R 2 | IC50 (nM) | IC50 (μM) | ||
| HCT116 | RKO | HT-29 | |||
| LB-1 |
|
9.22 | 0.92 ± 0.41 | 0.67 ± 0.16 | 2.94 ± 0.02 |
| LB-2 |
|
24.05 | 1.65 ± 0.32 | 1.69 ± 0.15 | 3.65 ± 0.52 |
| LB-3 |
|
17.52 | 1.54 ± 0.46 | 1.58 ± 0.33 | >5 |
| LB-4 |
|
242.50 | 2.60 ± 0.24 | 1.53 ± 0.28 | 3.89 ± 0.57 |
| LB-5 |
|
20.57 | 1.50 ± 0.17 | 1.43 ± 0.51 | 4.10 ± 0.44 |
| LB-6 |
|
385.3 | 2.36 ± 0.64 | 1.60 ± 0.14 | >5 |
| LB-7 |
|
124.8 | 2.63 ± 0.18 | 1.29 ± 0.35 | >5 |
| LB-8 |
|
5.25 | 3.91 ± 0.20 | 1.40 ± 0.05 | >5 |
| LB-9 |
|
15.85 | 1.78 ± 0.19 | 1.53 ± 0.07 | 2.76 ± 0.47 |
| LB-10 |
|
3.56 | 1.09 ± 0.11 | 3.21 ± 0.43 | 3.12 ± 0.42 |
| LB-11 |
|
27.42 | 1.73 ± 0.31 | 1.17 ± 0.05 | >5 |
| LB-12 |
|
51.61 | 1.78 ± 0.29 | 1.57 ± 0.36 | >5 |
| LA-13 |
|
18.76 | 2.12 ± 0.09 | 1.37 ± 0.57 | 3.24 ± 0.38 |
| AZD5438a | — | 19.21 | 1.38 ± 0.10 | 0.79 ± 0.54 | 4.10 ± 0.26 |
a
AZD5438 as the positive control.