Table 1.
Relative EC50 values of prexasertib in a panel of pediatric cancer cell lines.
| Cell Line | Histology | p53 status^ | EC50 (nM) | Max. inhibition† |
|---|---|---|---|---|
| Karpas-299 | anaplastic large-cell lymphoma | mutant | 0.9 | 100 ± 0.01 |
| COG-LL-317 | acute lymphoblastic leukemia | wild type | 2.6 | 100 ± 0.01 |
| CCRF-CEM | acute lymphoblastic leukemia | mutant | 3.0 | 100 ± 0.00 |
| MOLT-4 | acute lymphoblastic leukemia | wild type | 3.4 | 100 ± 0.01 |
| RS4;11 | acute lymphoblastic leukemia | wild type | 4.5 | 100 ± 0.00 |
| NALM-6 | acute lymphoblastic leukemia | wild type | 5.1 | 100 ± 0.00 |
| Kasumi-1 | acute myeloid leukemia | mutant | 3.5 | 97.6 ± 0.10 |
| SJCRH30 | alveolar rhabdomyosarcoma | mutant | 1.4 | 99.3 ± 0.04 |
| SJCRH30* | alveolar rhabdomyosarcoma | mutant | 2.9 | 96.8 ± 0.37 |
| Rh41 | alveolar rhabdomyosarcoma | mutant | 8.8 | 96.6 ± 0.51 |
| Rh41* | alveolar rhabdomyosarcoma | mutant | 5.5 | 92.2 ± 1.22 |
| RD | embryonal rhabdomyosarcoma | mutant | 22 | 87.0 ± 0.57 |
| RD* | embryonal rhabdomyosarcoma | mutant | 9.1 | 74.0 ± 2.27 |
| Rh18 | embryonal rhabdomyosarcoma | wild type | 2.9 | 88.6 ± 1.70 |
| A673* | Ewing’s sarcoma | mutant‡ | 5.2 | 75.9 ± 2.80 |
| CHLA-9 | Ewing’s sarcoma | wild type | 1.6 | 98.7 ± 0.20 |
| TC-71 | Ewing’s sarcoma | mutant‡ | 1.6 | 100 ± 0.00 |
| CHLA-10 | Ewing’s sarcoma | mutant | 1.7 | 99.3 ± 0.20 |
| CHLA-258 | Ewing’s sarcoma | wild type | 2.4 | 89.8 ± 0.30 |
| SJ-GBM2 | glioblastoma | mutant | 2.6 | 98.5 ± 0.13 |
| BT-12 | atypical teratoid/rhabdoid tumor | wild type | 6.6 | 80.2 ± 0.70 |
| CHLA-266 | malignant rhabdoid tumor | wild type | 15 | 55.5 ± 1.69 |
| CHLA-136 | neuroblastoma | wild type | 0.9 | 87.2 ± 1.02 |
| NB-EBc1 | neuroblastoma | wild type | 1.7 | 98.7 ± 0.12 |
| CHLA-90 | neuroblastoma | mutant | 3.7 | 91.9 ± 0.19 |
| NB-1643 | neuroblastoma | wild type | 4.8 | 97.6 ± 0.07 |
| Ramos-RA1 | non-Hodgkin’s lymphoma | mutant | 6.5 | 99.5 ± 0.01 |
| MG-63* | osteosarcoma | mutant‡ | 8.1 | 97.7 ± 0.18 |
*
calculated from 72h timepoint
^
p53 status previously reported in Carol H et al. Initial testing of the MDM2 inhibitor RG7112 by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer 2013;60(4):633–41.
‡
p53 status previously reported in Ottaviano L et al. Molecular characterization of commonly used cell lines for bone tumor research: a trans-European EuroBoNet effort. Genes Chromosomes Cancer 2010;49(1):40–51.
†
Inhibition achieved at 1 μM prexasertib, calculated as (1-(treated/control)*100%) and reported as %Max Inhibition ± SEM; complete curves shown in Supplementary Fig. S1.