FIDAS-5

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FIDAS-5 有效地与 S-腺苷甲硫氨酸 (SAM) 竞争 MAT2A 结合。 FIDAS-5 具有抗癌活性。 FIDAS-5 是一种有效的口服活性蛋氨酸 S-腺苷转移酶 2A (MAT2A) 抑制剂，IC50 为 2.1 μM。FIDAS-5 诱导细胞周期抑制剂 p21WAF1/CIP1 的表达。 FIDAS-5（3 μM；36 小时）处理可降低 LS174T 细胞中 S-腺苷甲硫氨酸（SAM）和 S-腺苷高半胱氨酸（SAH）的水平。FIDAS-5（3 μM；7 天；LS174T 细胞）处理显着抑制LS174T细胞的增殖。

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.?

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.

Animal Model:16 athymic nude mice injected with HT29 CRC cellsDosage:20 mg/kg Administration:Oral gavage; daily; for two weeks Result:Significantly inhibited the growth of xenograft tumors.

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Others

Other Targets

MAT2A

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1391934-98-7

261.72

C15H13ClFN

>98% (HPLC)

DMSO:125 mg/mL (477.61 mM; Need ultrasonic)

CNC1=CC=C(/C=C/C2=C(F)C=CC=C2Cl)C=C1

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(-20℃)

With Ice Pack

≥ 2 years