Table 4.
Effects of various targeted drugs on growth of human MC lines
| Cell line | Avapritinib (BLU-285) IC50 (µM) | Nintedanib (BIBF-1120) IC50 (µM) | Midostaurina (PKC412) IC50 (µM) | Cladribine (2CdA) IC50 (µM) |
|---|---|---|---|---|
| HMC-1.1 | 0.1-0.25 | 0.001-0.01 | 0.25-0.5 | 1-5 |
| HMC-1.2 | 0.1-0.25 | 0.25-0.5 | 0.1-0.25 | 0.01-0.1 |
| ROSAKIT WT | 0.1-0.25 | 0.01-0.1 | 0.1-0.25 | 0.01-0.1 |
| ROSAKIT D816V | 1-5 | 0.5-1 | 0.25-0.5 | 0.01-0.1 |
| ROSAKIT K509I | 0.1-0.25 | 0.01-0.1 | 0.1-0.25 | 0.01-0.1 |
| MCPV-1.1 | 5-10 | 1-5 | 1-5 | 1-5 |
| MCPV-1.2 | 1-5 | 0.01-0.1 | 0.5-1 | 0.5-1 |
| MCPV-1.3 | 5-10 | 1-5 | 1-5 | 1-5 |
| MCPV-1.4 | 5-10 | 1-5 | 0.5-1 | 1-5 |
Mast cell lines were incubated in control medium and medium containing various concentrations of avapritinib, nintedanib, midostaurin or cladribine at 37°C for 48 hours. Then, proliferation was determined by measuring uptake of 3H-thymidine and IC50 ranges were calculated from three independent experiments. Abbreviations: MC, Mast Cells; IC50, Half Maximal Inhibitory Concentration; µM, Micromolar.
a
IC50 values for midostaurin in HMC-1 cells confirmed the available literature [35].