FIDAS-5

SKU: orb1219294

Description

FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities. FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM.FIDAS-5 induces the expression of cell cycle inhibitor, p21WAF1/CIP1. FIDAS-5 (3 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells.FIDAS-5 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells. FIDAS-5 (3 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. Mice are treated with FIDAS-5 (20 mg/kg) for 1 week. The liver SAM levels are significantly reduced.FIDAS-5 (20 mg/kg; oral gavage; daily; for two weeks; athymic nude mice) treatment significantly inhibits the growth of xenograft tumors, with minimal difference in body weight.

Key Properties

• CAS Number: 1391934-98-7
• MW: 261.72
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₃ClFN
• SMILES: CNC1=CC=C(/C=C/C2=C(F)C=CC=C2Cl)C=C1
• Target: MAT2A
• Solubility: DMSO:125 mg/mL (477.61 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: 16 athymic nude mice injected with HT29 CRC cells. Dosage: 20 mg/kg. Administration: Oral gavage; daily; for two weeks. Result: Significantly inhibited the growth of xenograft tumors.
  Read more...
• In Vitro:
  Cell Viability Assay Cell line: LS174T colorectal cancer (CRC) cells. Concentration: 3 μM. Incubation time: 7 days. Result: Significantly inhibited the proliferation of LS174T cells.
  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

Quick Database Links

Gene Symbol

MAT2A