MAT2A Inhibitor II, FIDAS-5

Name: MAT2A Inhibitor II, FIDAS-5
Brand: MM

Synonym(s):

MAT2A Inhibitor II, FIDAS-5, FIDAS5, Methionine S-Adenosyltransferase 2A Inhibitor II, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline, Methionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline

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About This Item

Empirical Formula (Hill Notation):

C₁₅H₁₃ClFN

CAS Number:

1391934-98-7

Molecular Weight:

261.72

MDL number:

MFCD32671894

UNSPSC Code:

12352200

NACRES:

NA.77

Assay

≥98% (HPLC)

Quality Level

100

form

semisolid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

SMILES string

Fc1c(c(ccc1)Cl)\C=C\c2ccc(cc2)NC

InChI key

KXVXICBOMOGFMH-JXMROGBWSA-N

General description

A cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 that is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM (S-adenosylmethionine) synthesis both in cell-free (IC₅₀ = 2.1 µM with FIDAS-5 vs. 4.9 µM with FIDAS-3; [L-Met] = [ATP] = 1 mM, [MAT2A] = 10 µg/mL; 20 min FIDAS preincubation prior to 30 min reaction) and cell-based (64% and 56% decrease of SAM and SAH level, respectively, in LS174T cells after 36 h treatment with either 3 µM FIDAS-5 or 10 µM FIDAS-3) assays. FIDAS-5 at 3 µM is shown to completely inhibit the proliferation of LS174T CRC (colorectal cancer) for up to 7 d in vitro and, when administered orally, effectively suppress HT29 CRC tumor expansion in mice in vivo (by 58% on d 18 post HT29 xenograft; 20 mg/kg/day starting d 4). Computer-aided in silico modeling predicts that FIDAS-3 & -5 target SAM-binding pocket at the interface of MAT2A dimer and in vitro binding studies reveals FIDAS-3 effectively competes against SAM for MAT2A binding.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MAT2A

Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Zhang, W., et al. 2013. ACS Chem. Biol.8, 796.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Global Trade Item Number

SKU	GTIN
5.04173.0001	04055977263831

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