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
Size Price / USD Stock Quantity
5MG 235 Get Quote
10MG 348 Get Quote
25MG 584 Get Quote
50MG 831 Get Quote
100MG 1134 Get Quote
500MG 2268 Get Quote
1G Get Quote Get Quote

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.
  • In Vitro
    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.AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line.AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block.AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways.
  • In Vivo
    AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2247919-28-2
  • Formula Weight
    442.31
  • Molecular Formula
    C21H13Cl2N3O2S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (113.04 mM)
  • 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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