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Merck

5.04599

ML243

Synonym(s):

ML243, Cancer Stem Cell Inhibitor, ML243, ( E)-N-(4,5-Dihydrothiazol-2-yl)-3-(4-ethylphenyl)acrylamide, (2 E)-N-(4,5-Dihydro-1,3-thiazol-2-yl)-3-(4-ethylphenyl)prop-2-enamide

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About This Item

Empirical Formula (Hill Notation):
C14H16N2OS
CAS Number:
1426576-80-8
Molecular Weight:
260.35
UNSPSC Code:
12352200

Key Documents

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assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Cell permeable: yes

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, biologically stable, 4-ethyl substituted cinnamide analog that selectively exerts an inhibitory effect on breast cancer stem-like cells (EC50 = 2 µM for epithelial-to-mesenchymal transition; HMLE_shEcad). Exhibits ~32-fold greater selectivity over isogenic control cells (EC50 = 64 µM; HMLE cell line expressing shRNA against eGFPcells; HMLE_sh_eGFP). Displays desirable aqueous solubility (~11.5 µM in PBS, pH 7.4) and excellent stability in human plasma and in glutathione solution. Shown to block the binding to a radio-labeled ligand to the Adenosine A2A Receptor (IC50 = 10 µM), but does not affect 68 other targets studied.

Other Notes

Germain, A.R., et al. 2013. Bioorg. Med. Chem. Lett.23, 1834.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Use only fresh DMSO for reconstitution.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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