| Bioactivity | AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM[1]. |
| Invitro | AAPK-25 inhibits HCT-116, Calu6, A549 and MCF-7 cells growth with IC50s of 0.4, 5.3, 11.6, and 2.3 μM, respectively[1].AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line[1].AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block[1].AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways[1]. |
| Name | AAPK-25 |
| CAS | 2247919-28-2 |
| Formula | C21H13Cl2N3O2S |
| Molar Mass | 442.32 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |