Table 1.
Anti-proliferative activity of GZD824 in leukemia cells harboring gene fusions of FLT3, FGFR1 and PDGFRα
| IC50 (nM, AV ± SD) |
GZD824 (HQP1351) |
Quizaritinib (AC220) |
Gilteritinib (ASP2215) |
|---|---|---|---|
| MV411Flt3-ITD | 2.00 ± 1.10 | 1.07 ± 0.32 | 3.34 ± 0.91 |
| MOLM-13Flt3-ITD | 6.01 ± 6.10 | 5.67 ± 9.29 | 9.35 ± 2.23 |
| KG1FGFR1OP2-FGFR1 | 3.66 ± 1.93 | 1019.23 ± 571.53 | 820.58 ± 175.95 |
| EOL-1PDGFRα | 7.56 ± 2.73 | 1505.50 ± 450.77 | 719.08 ± 129.53 |
| NB4Flt3-WT | 1384.25 ± 1150.50 | 1990.00 ± 889.96 | 118.38 ± 674.43 |
| HL60Flt3-WT | 921.80 ± 209.65 | 1167.33 ± 72.13 | 688.75 ± 397.77 |
| U937Flt3-WT | 1167.00 ± 104.54 | 1430.60 ± 246.37 | 1134.62 ± 330.38 |
| THP1Flt3-WT | 2014.40 ± 414.56 | >1000.00 | >1000.00 |
| MEG01Flt-WT | 388.98 ± 151.74 | 3307.00 ± 1563.70 | 1137.64 ± 518.86 |
| MOLT4Flt3-WT | 245.69 ± 139.45 | 1946.78 ± 1749.86 | 891.85 ± 316.20 |
The anti-proliferative activities of the compounds were evaluated with a CCK-8 assay. The data presented are means from at least four independent experiments.