PFK-158

SKU: orb1223291

Description

PFK-158, also known as ACT-PFK-158, is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) with potential antineoplastic activity. Upon administration, PFKFB3 inhibitor PFK-158 binds to and inhibits the activity of PFKFB3, which leads to the inhibition of both the glycolytic pathway in and glucose uptake by cancer cells. This prevents the production of macromolecules and energy that causes the enhanced cellular proliferation in cancer cells as compared to that of normal, healthy cells. Depriving cancer cells of nutrients and energy leads to the inhibition of cancer cell growth.(In Vitro):PFK-158 (10 μM ; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%).PFK-158 (0-10 μM ; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively.PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs.(In Vivo):PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model.

Key Properties

• CAS Number: 1462249-75-7
• MW: 328.29
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₁F₃N₂O
• SMILES: c12c(ccc(n1)C(F)(F)F)ccc(c2)/C=C/C(=O)c1ccncc1
• Target: GPR
• Solubility: DMSO : ≥ 30 mg/mL; 91.38 mM

Bioactivity

• In Vivo:
  PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model. Animal model: Female athymic nude mice (nu/nu) (5-6 weeks old) injected with HeyA8MDR cells. Dosage: 15 mg/kg. Administration: Intraperitoneal injection; once a week; for 4 weeks. Result: A marked reduction of tumor growth was observed in the combination treatment.
• In Vitro:
  PFK-158 (10 μM; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%). PFK-158 (0-10 μM; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels. PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively. PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs. Apoptosis Analysis Cell line: OV2008 and C13 cells. Concentration: 10 μM. Incubation time: 24 hours. Result: Combined with Carboplatin (CBPt) treatment resulted in significant increase in apoptosis. Western blot analysis. Cell line: C13 and HeyA8MDR cells. Concentration: 0 μM, 5 μM, 10 μM. Incubation time: 24 hours. Result: Demonstrated a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.

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

PFK158 | PFK 158 | PFK158 | ACTPFK158

Quick Database Links

Gene Symbol

GPR