LF3

Alias: LF-3;LF 3
Cat No.:V2725 Purity: ≥98%
LF3 is a specific antagonist of the β-Catenin/TCF4 interaction with antitumor activity; it acts by disrupting the interaction between β-catenin and TCF4 with an IC50of 1.65 μM.
LF3 Chemical Structure CAS No.: 664969-54-4
Product category: Wntbeta-catenin
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

LF3 is a specific antagonist of the β-Catenin/TCF4 interaction with antitumor activity; it acts by disrupting the interaction between β-catenin and TCF4 with an IC50 of 1.65 μM. LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. The self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners, as examined by sphere formation of colon and head and neck cancer stem cells under nonadherent conditions. LF3 inhibits Wnt/β-catenin signaling, but does not interfere with E-cadherin/β-catenin-mediated cell-cell adhesion.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In cells containing exogenous reporters and colon cancer cells with high endogenous Wnt activity, LF3 suppresses Wnt/β-catenin signals. Moreover, LF3 inhibits the overexpression of Wnt target genes, high cell motility, and cell-cycle progression in cancer cells that are connected to Wnt signaling. LF3 does not, however, impair cadherin-mediated cell-cell adhesion or result in cell death. Surprisingly, LF3 inhibits cancer stem cells' ability to self-renew in ways that depend on concentration[1].
ln Vivo
LF3 inhibits tumor growth and promotes differentiation in a colon cancer mouse xenograft model. When LF3 at 50 mg/kg is administered to mice with GFPhigh cells, tumor growth is markedly inhibited. The normal histology of mice's guts is not affected by LF3 treatment[1].
Animal Protocol
50 mg/kg; i.v. injection
NOD/SCID mice
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H24N4O2S2
Molecular Weight
416.56
CAS #
664969-54-4
Related CAS #
664969-54-4
SMILES
S=C(N1CCN(C/C=C/C2=CC=CC=C2)CC1)NC3=CC=C(S(=O)(N)=O)C=C3
Synonyms
LF-3;LF 3
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 83 mg/mL (199.3 mM)
Water:<1 mg/mL
Ethanol: 5 mg/mL (12.0 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4006 mL 12.0031 mL 24.0061 mL
5 mM 0.4801 mL 2.4006 mL 4.8012 mL
10 mM 0.2401 mL 1.2003 mL 2.4006 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • LF3

    Compound LF3 disrupts the interaction between β-catenin and TCF4.Cancer Res.2016 Feb 15;76(4):891-901.
  • LF3

    LF3 specifically inhibits Wnt/β-catenin signaling in cells.Cancer Res.2016 Feb 15;76(4):891-901.
  • LF3

    LF3 inhibits Wnt/β-catenin signaling in colon cancer cells.Cancer Res.2016 Feb 15;76(4):891-901.
  • LF3

    LF3 inhibits the self-renewal of colon CSCs.Cancer Res.2016 Feb 15;76(4):891-901.
  • LF3

    LF3 induces differentiation of mouse salivary gland CSCs.Cancer Res.2016 Feb 15;76(4):891-901.
  • LF3

    LF3 reduces tumor growth and induces differentiation of colon CSCs in vivo.Cancer Res.2016 Feb 15;76(4):891-901.
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