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PFK-015

CAS No. 4382-63-2

PFK-015( PFK015 | PFK 015 | PFK015. )

Catalog No. M18553 CAS No. 4382-63-2

PFK-015 is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PFK-015
  • Note
    Research use only, not for human use.
  • Brief Description
    PFK-015 is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).
  • Description
    PFK-015 is a potent inhibitor of PFKFB3. The preliminary results in a U87GM xenograft model have shown that PFK-015 has comparable activity to Temozolomide. PFK-015 inhibits glucoseuptake by tumors.
  • In Vitro
    PFK-015 inhibits tumor growth in a dose-dependent manner in esophageal cancer cell line in vitro. PFK-015 (0-5 μM) increases HIF-1α mediated PD-L1 transcriptional activity.PFK-015 induces the expression of tumor PD-L1 via the phos-PFKFB3/HIF-1a axis.PFK-015 potently inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM.PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines and suppresses glucose uptake in cancer cells.
  • In Vivo
    PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models.PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression.PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 + T cells.PFK-015 enhances the efficacy of ESCC by enhancing CD8 + T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG.PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance.
  • Synonyms
    PFK015 | PFK 015 | PFK015.
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    PFKFB3
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    4382-63-2
  • Formula Weight
    260.29
  • Molecular Formula
    C17H12N2O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 25.2 mg/mL 96.82 mM; H2O : < 0.1 mg/mL
  • SMILES
    C(=O)(/C=C/c1nc2c(cc1)cccc2)c1ccncc1
  • Chemical Name
    (E)-3-(pyridin-3-yl)-1-(quinolin-3-yl)prop-2-en-1-one

Shipping & Storage Information

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

Reference

1. Clem BF, et al. Mol Y Ther. 2013, 12(8), 1461-1470.
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