PFK-015

SKU: orb1222258

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.

Key Properties

• CAS Number: 4382-63-2
• MW: 260.29
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂N₂O
• SMILES: C(=O)(/C=C/c1nc2c(cc1)cccc2)c1ccncc1
• Target: PFKFB3
• Solubility: DMSO : 25.2 mg/mL 96.82 mM; H2O : < 0.1 mg/mL

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PFK015 | PFK 015 | PFK015.

Quick Database Links

Gene Symbol

PFKFB3