AAPK-25

• CAT Number: I018696
• CAS Number: 2247919-28-2
• Molecular Formula: C₂₁H₁₃Cl₂N₃O₂S
• Molecular Weight: 442.32
• Purity: ≥95%

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].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].AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model[1].

Reference

[1]. Qi B, et al. Discovery of inhibitors of Aurora/PLK targets as anti-cancer agents. J Med Chem. 2019 Aug 5.