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AAPK-25

CAS No. 2247919-28-2

AAPK-25 ( —— )

Catalog No. M26043 CAS No. 2247919-28-2

AAPK-25, a potent and selective dual inhibitor of Aurora/PLK, causes mitotic delay and cell arrest in prometaphase, via phosphorylation of the biomarker histone H3Ser10, followed by a surge in apoptosis.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    AAPK-25
  • Note
    Research use only, not for human use.
  • Brief Description
    AAPK-25, a potent and selective dual inhibitor of Aurora/PLK, causes mitotic delay and cell arrest in prometaphase, via phosphorylation of the biomarker histone H3Ser10, followed by a surge in apoptosis.
  • Description
    AAPK-25, a potent and selective dual inhibitor of Aurora/PLK, causes mitotic delay and cell arrest in prometaphase, via phosphorylation of the biomarker histone H3Ser10, followed by a surge in apoptosis. AAPK-25 targets Aurora A, Aurora B, and Aurora C with Kd values ??ranging from 23-289 nM, and PLK1, PLK2, and PLK3 with Kd values ??ranging from 55-456 nM. AAPK-25 has antitumor activity.(In Vitro):AAPK-25 inhibited HCT-116, Calu6, A549, and MCF-7 cells growth (IC50s: 0.4, 5.3, 11.6, and 2.3 μM). AAPK-25 dose-dependently induced apoptosis in HCT-116 cell line.(In Vivo):In the BALB/c nude mice tumor xenograft model, AAPK-25 enhanced the survival rate.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2247919-28-2
  • Formula Weight
    442.3
  • Molecular Formula
    C21H13Cl2N3O2S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    Clc1ccc(cc1Cl)C(=O)Nc1ccc2cc(ccc2c1)C(=O)Nc1nccs1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Pacold ME, et al. A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate [published correction appears in Nat Chem Biol. 2016 Jul 19;12 (8):656]. Nat Chem Biol. 2016;12(6):452-458.
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