Table 2. IC50 Values for Various Types of HER TKIs, CDK, C-MET, SRC and STAT3 Inhibitors.
| IC50 value (µM) |
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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Erlotinib (reversible EGFR inhibitor) |
Lapatinib (reversible EGFR/HER2 inhibitor) |
Neratinib (irreversible EGFR/HER2 inhibitor) |
Afatinib (irreversible EGFR/HER2/HER4 inhibitor) |
Palbociclib (CDK4/CDK6 inhibitor) |
Dinaciclib (CDK1/CDK2/ CDK5/CDK9 inhibitor) |
Ribociclib (CDK4/CDK6 inhibitor) |
Capmatinib (c-MET inhibitor) |
Dasatinib (Abl/Src/c-Kit inhibitor) |
Stattic (STAT3 inhibitor) |
|||||||||||
| FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | FBS 2% | FBS 10% | |
| HGC-27 | > 10.00 | > 10.00 | 3.35 ± 0.15 | > 10.00 | 2.4 ± 0.53 | 2.71 ± 0.69 | 3.05 ± 0.34 | 3.26 ± 0.15 | 2.21 ± 1.55 | 3.73 ± 1.18 | 0.009 ± 0.001 | 0.01 ± 0 | > 10.00 | > 10.00 | > 10.00 | > 10.00 | 0.04 ± 0.001 | 4.89 ± 1.72 | 1.67 ± 0.17 | 1.69 ± 0.18 |
| AGS | 7.22 ± 0.88 | > 10.00 | > 10.00 | > 10.00 | 0.17 ± 0.08 | 2.43 ± 1.03 | 0.96 ± 0.08 | 3.97 ± 0.75 | 4.52 ± 1.12 | > 10.00 | 0.009 ± 0.000 | 0.009 ± 0.001 | > 10.00 | > 10.00 | > 10.00 | > 10.00 | 0.03 ± 0.001 | 0.24 ± 0.31 | 1.23 ± 0.01 | 2.29 ± 0.18 |
| FU97 | 1.48 ± 0.60 | 2.95 ± 0.84 | 0.48 ± 0.27 | 2.48 ± 0.76 | 0.46 ± 0.12 | 0.04 ± 0.02 | 0.26 ± 0.07 | 0.66 ± 0.13 | 0.007 ± 0.01 | 0.05 ± 0.03 | 0.004 ± 0.00 | 0.005 ± 0.00 | > 10.00 | > 10.00 | > 10.00 | > 10.00 | 0.002 ± 0.00 | 0.12 ± 0.008 | 0.38 ± 0.09 | 0.83 ± 0.28 |
| MKN1 | 0.06 ± 0.02 | 4.19 ± 2.72 | 0.15 ± 0.06 | 3.98 ± 0.67 | 0.03 ± 0.008 | 0.13 ± 0.06 | 0.015 ± 0.001 | 0.86 ± 0.10 | 5.36 ± 0.81 | > 10.00 | 0.023 ± 0.001 | 0.003 ± 0.001 | > 10.00 | > 10.00 | > 10.00 | > 10.00 | 0.004 ± 0.001 | 0.015 ± 0.004 | 0.77 ± 0.11 | 1.67 ± 0.22 |
| MKN74 | 8.87 ± 1.08 | > 10.00 | 1.22 ± 0.22 | 8.39 ± 0.04 | 2.06 ± 0.21 | 2.57 ± 0.18 | 3.33 ± 0.10 | 4.32 ± 0.20 | 4.03 ± 0.13 | 3.94 ± 0.22 | 0.011 ± 0.001 | 0.014 ± 0.001 | > 10.00 | > 10.00 | > 10.00 | > 10.00 | 8.34 ± 0.77 | > 10.00 | 2.21 ± 0.04 | 2.42 ± 0.46 |
| NCI-N87 | 0.89 ± 0.17 | 0.23 ± 0.17 | 0.004 ± 0.001 | 0.013 ± 0.001 | 0.001 ± 0.17 | 0.001 ± 0.001 | 0.002 ± 0.19 | 0.003 ± 0.00 | 2.90 ± 2.01 | 7.64 ± 0.17 | 0.008 ± 0.001 | 0.001 ± 0.001 | > 10.00 | > 10.00 | > 10.00 | > 10.00 | 0.12 ± 0.001 | 0.19 ± 0.07 | 0.87 ± 0.11 | 1.39 ± 0.05 |
HER: human epidermal growth factor receptor family; CDK: cyclin dependent kinase; TKI: tyrosine kinase inhibitor; FBS: fetal bovine serum; IC50: 50% inhibitory concentration; EGFR: epidermal growth factor receptor; c-MET: hepatocyte growth factor receptor; STAT3: signal transducer and activator of transcription 3.