FIDAS-5 (C09-1133-710)

FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC 50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activitiesIn VitroFIDAS-5 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells. ?/nFIDAS-5 (3 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. And FIDAS-5 induces the expression of cell cycle inhibitor, p21 WAF1/CIP1. ?/nFIDAS-5 (3 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: LS174T colorectal cancer (CRC) cells Concentration: 3 μM Incubation Time: 7 days Result: Significantly inhibited the proliferation of LS174T cells.In VivoFIDAS-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 . ?/nMice are treated with FIDAS-5 (20 mg/kg) for 1 week. The liver SAM levels are significantly reduced . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:SolidIC50& Target:IC50: 2.1 μM (Methionine S-adenosyltransferase 2A (MAT2A)). Specification: 0.98 Molecular Formula: C15H13ClFN Molecular Weight: 261.72 PubChem CID: 57521314 Isomeric SMILES: CNC1=CC=C(C=C1)/C=C/C2=C(C=CC=C2Cl)F