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504173 MAT2A Inhibitor II, FIDAS-5 - CAS 1391934-98-7 - Calbiochem

MAT2A Inhibitor II, FIDAS-5 - CAS 1391934-98-7 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Methionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline

Primary Target: MAT2A
504173
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
1391934-98-7C₁₅H₁₃ClFN

Products

KatalógusszámCsomagolás Menny./csomag
5.04173.0001 Üvegpalack 10 mg
Description
OverviewA cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 (Cat. No. 681677) that competes against SAM for MAT2A binding and is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM synthesis both in cell-free assays (IC50 = 2.1 µM) and in LS174T colorectal cancer (CRC) cultures (3 µM). FIDAS-5 at 3 µM is shown to completely inhibit the proliferation of LS174T for up to 7 d in vitro and effectively suppress HT29 CRC tumor expansion in mice in vivo (20 mg/kg/day p.o.).
Catalogue Number504173
Brand Family Calbiochem®
SynonymsMethionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline
References
ReferencesZhang, W., et al. 2013. ACS Chem. Biol. 8, 796.
Product Information
CAS number1391934-98-7
FormYellow semi-solid
Hill FormulaC₁₅H₁₃ClFN
Chemical formulaC₁₅H₁₃ClFN
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetMAT2A
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.04173.0001 04055977263831

Documentation

MAT2A Inhibitor II, FIDAS-5 - CAS 1391934-98-7 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

MAT2A Inhibitor II, FIDAS-5 - CAS 1391934-98-7 - Calbiochem Certificates of Analysis

TitleLot Number
504173

References

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

Brochure

Title
New Products Flyer- Feb 2014 - Vol 1
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision18-June-2020 JSW
SynonymsMethionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline
DescriptionA cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 (Cat. No. 681677) 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.
FormYellow semi-solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1391934-98-7
Chemical formulaC₁₅H₁₃ClFN
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesZhang, W., et al. 2013. ACS Chem. Biol. 8, 796.