FR054

SKU: orb1940193

Description

FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect. FR054 induces in different breast cancer cells a dramatic decrease in cell proliferation and survival.(In Vivo):The effect of FR054 occurs through PGM3 inhibition instead of other off-target effects. FR054 (0.5-1 mM, 24-48 h) induces an early proliferation arrest followed by a marked cell death increase in breast cancer cells and induces apoptosis. FR054 (250 μM, 24 h) treatment efficiently affects both N- and O-glycosylation levels in MDA-MB-231 cells. FR054 induces endoplasmic reticulum stress and ROS-dependent apoptotic cell death .

Key Properties

• CAS Number: 35954-65-5
• MW: 657.6
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₇N₂O₁₆
• SMILES: CC(OC[C@H]([C@H]1OC(C)=O)O[C@@H]2OC(C)=N[C@@H]2[C@H]1OC(C)=O)=OCC(OC[C@H]([C@H]1OC(C)=O)O[C@@H]2OC(C)=N[C@@H]2[C@H]1OC(C)=O)=O
• Solubility: In Vitro: DMSO : 100 mg/mL (303.67 mM)

Bioactivity

• In Vivo:
  Animal model: Mice were subcutaneously injected with MDA-MB-231 cells. Dosage: 1000 mg/kg. Administration: IP, single or fractionated dose (twice a day 500 mg/kg/dose). Result: Appears to have an In vivo antitumor efficacy that is higher when administered twice a day compared to single administration.
  Read more...
• In Vitro:
  Cell Viability Assay Cell line: MDA-MB-231 cells. Concentration: 0.5-1 mM. Incubation time: 48 h. Result: Reduced viability and a significant increase of the apoptosis as compared to the control clone.
  Read more...

Storage & Handling

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