GLPBio

LF3

Catalog No.: GC32763Purity:>99.50%
COASDSData Sheet
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.

Products are for research use only. Not for human use. We do not sell to patients.

LF3
Cas No.: 664969-54-4
10mM (in 1mL DMSO)In Stock
$61.00
1
5mgIn Stock
$56.00
1
10mgIn Stock
$72.00
1
25mgIn Stock
$161.00
1
50mgIn Stock
$258.00
1
100mgIn Stock
$478.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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Description

LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.

LF3 inhibits Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppresses features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes. However, LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners[1].

LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumor growth is significantly reduced when mice with GFPhigh cells are treated with LF3 at 50 mg/kg. LF3 treatment does not disturb the normal histology of the gut of mice[1].

[1]. Fang L, et al. A Small-Molecule Antagonist of the β-Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis. Cancer Res. 2016 Feb 15;76(4):891-901.

Protocol

Cell experiment:

LF3 is dissolved in DMSO to a concentration of 50 mM and diluted with culture medium. Two colon cancer cell lines (HCT116 and HT29) and a breast cancer cell line (MCF7) are treated with LF3 (0, 30, 60 μM) for 24 hours and labeled with BrdUrd for 4 to 5 hours to detect proliferating cells[1].

Animal experiment:

Mice: Unsorted GFPlow and GFPhigh SW480 cells are subcutaneously injected into the back skin of NOD/SCID mice. Tumor growth is monitored over a period of 45 days. For therapy, LF3 is administered i.v. at 50 mg/kg body weight for three rounds over 5 consecutive days, with 2-day breaks[1].

References:

[1]. Fang L, et al. A Small-Molecule Antagonist of the β-Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis. Cancer Res. 2016 Feb 15;76(4):891-901.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
664969-54-4
SMILES
S=C(N1CCN(C/C=C/C2=CC=CC=C2)CC1)NC3=CC=C(S(=O)(N)=O)C=C3
Molecular Formula
C20H24N4O2S2
Molecular Weight
416.56
Solubility
DMSO : ≥ 32 mg/mL (76.82 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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