详情描述
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities.
Product information
CAS Number: 1391934-98-7
Molecular Weight: 261.72
Formula: C15H13ClFN
Chemical Name: FIDAS-5
Smiles: CNC1C=CC(/C=C/C2=C(F)C=CC=C2Cl)=CC=1
InChiKey: KXVXICBOMOGFMH-JXMROGBWSA-N
InChi: InChI=1S/C15H13ClFN/c1-18-12-8-5-11(6-9-12)7-10-13-14(16)3-2-4-15(13)17/h2-10,18H,1H3/b10-7+
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 125 mg/mL (477.61 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
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. And 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.
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. Mice are treated with FIDAS-5 (20 mg/kg) for 1 week. The liver SAM levels are significantly reduced.
References:
- Zhang W, et al. Fluorinated N,N-dialkylaminostilbenes repress colon cancer bytargeting methionine S-adenosyltransferase 2A. ACS Chem Biol. 2013 Apr 19;8(4):796-803.
Products are for research use only. Not for human use.