Table 2.
Cytotoxic IC50 values of HAA2020, the eleven inhibitors and their combinations in HL60 cells (24 h, nM).
| No. | Inhibitor | Targets | IC50 nM | IC50 (nM) Combination HAA2020/Inhibitor a (50:1) | CI b at Fa = 0.9 |
|---|---|---|---|---|---|
| 1 | PHA-767491 | CDK1/2,CDK5, Cdc7/CDK9, GSK3-β,MK2 PLK1, CHK2 | 26.1 ± 3.8 | 21.8 ± 3.2 | 0.991 |
| 2 | Dinaciclib | CDK1, CDK2, CDK5, CDK9 | 8.2 ± 0.3 | 4.9 ± 1.3 | 0.628 |
| 3 | ON123300 | CDK4, Ark5, PDGFRβ, FGFR RET, Fyn | 37.3 ± 3.5 | 1872.5 ± 45.9 | >1 |
| 4 | AMG 925 | CDK4/FLT3 | 54.4 ± 7.7 | 3355 ± 347.8 | >1 |
| 5 | KW2449 | FLT3, EGFR, FGFR1, Bcr-Abl PDGFRβ, IGF-1R | 56.5 ± 10.8 | 2535.5 ± 318.9 | >1 |
| 6 | AZD2932 | FLT3, c-Kit, VEGFR, PDGFRβ | 15.2 ± 3.1 | 2394 ± 380.4 | >1 |
| 7 | Dasatinib | c-Kit, Abl, Src | 12.1 ± 2.9 | 3036 ± 181.1 | >1 |
| 8 | BGJ398 | Kit, FGFR, VEGFR2, Abl, Fyn, Lck, Lyn, Yes | 16.2 ± 1.7 | 2952.5 ± 170.6 | >1 |
| 9 | Saracatinib | EGFR, Src, Yes, Fyn, Lyn, Blk, Fgr, Lck, Abl | 16.8 ± 1.2 | 1821.5 ± 40.3 | >1 |
| 10 | Lapatinib | EGFR, HER2 | 12.1 ± 2.0 | 2383.5 ± 245.3 | >1 |
| 11 | Taselisib | PI3Kα/δ/γ | 7.9 ± 0.4 | 2647 ± 203.6 | >1 |
| HAA 2020 | VEGFR2, EGFR, HER2 | 1814.5 ± 230.8 | - | - |
a: inhibitors 1–11. b: Combination index. (-): not applicable. Data are represented as mean ± SD (n = 3). Experiment was repeated 3×. IC50 of some combinations is more than 100 nM because the IC50 of HAA2020 alone is more than 100 nM.