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 activities.
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Product Description
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 activities
In Vitro
FIDAS-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 Vivo
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 . ?\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.
