FIDAS-3

  Cat. No.:  DC57081   Featured
Chemical Structure
1266684-01-8
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Field of application
FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities.
Cas No.: 1266684-01-8
Chemical Name: Fidas-3
Synonyms: FIDAS-3;4-[2-(2,6-Difluorophenyl)ethenyl]-N,N-dimethylaniline;BDBM102424;NSC783761;Fluorinated N,N-Dialkylaminostilbenes 3;(E)-4-(2,6-Difluorostyryl)-N,N-dimethylaniline;trans-2,6-difluoro-4'-(N,N-dimethylamino)stilbene;4-[(E)-2-(2,6-difluorophenyl)ethenyl]-N,N-dimethylaniline
SMILES: FC1C([H])=C([H])C([H])=C(C=1/C(/[H])=C(\[H])/C1C([H])=C([H])C(=C([H])C=1[H])N(C([H])([H])[H])C([H])([H])[H])F
Formula: C16H15F2N
M.Wt: 259.2938
Purity: >98%
Sotrage: 4°C, protect from light
Publication: [1]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803. [2]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes for Wnt pathway inhibition and colon cancer repression. J Med Chem. 2011 Mar 10;54(5):1288-97.
Description: FIDAS-3 is a stilbene derivative and is a potent Wnt inhibitor with an IC50 of 4.9 μM for methionine S-adenosyltransferase 2A (MAT2A). FIDAS-3 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-3 has anticancer activities[1][2].
Target: IC50: 4.9 μM (Methionine S-adenosyltransferase 2A (MAT2A))[1]
In Vivo: FIDAS-3 (20 mg/kg; intraperitoneal injection; daily; for one months; C57BL/6J athymic nude mice) treatment significantly inhibits the growth of xenograft tumors[2]. Animal Model: C57BL/6J athymic nude mice (6-8 week) injected with LS174 cells[2] Dosage: 20 mg/kg Administration: Intraperitoneal injection; daily; for one months Result: Significantly inhibited the growth of xenograft tumors.
In Vitro: FIDAS-3 (3 μM; 7 days; LS174T cells) treatment significantly inhibits the proliferation of LS174T cells[1]. FIDAS-3 (3-10 μM) treatment inhibits the expression of c-Myc and cyclinD1 in LS174T CRC cells. And FIDAS-3 induces the expression of cell cycle inhibitor, p21WAF1/CIP1[1]. FIDAS-3 (10 μM; 36 h) treatment reduces the levels of both S-adenosylmethionine (SAM) and S-adenosylhomocysteine (SAH) in LS174T cells[1]. Cell Viability Assay[1] Cell Line: LS174T colorectal cancer (CRC) cells Concentration: 3 μM Incubation Time: 7 days Result: Significantly inhibited the proliferation of LS174T cells.
References: [1]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer by targeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803. [2]. Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes for Wnt pathway inhibition and colon cancer repression. J Med Chem. 2011 Mar 10;54(5):1288-97.
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