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LF3

Cat. No. M4866
LF3 Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 85  USD85 In stock
25mg USD 175  USD175 In stock
50mg USD 300  USD300 In stock
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Quality Control
Biological Activity

In vitro: 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. LF3 blocks the expression of a series of Wnt target genes in Wnt-addicted colon cancer cells. It inhibits proliferation of Wnt-addicted colon cancer cells through induction of cell-cycle arrest and also inhibits self-renewal capacity of CSCs. In vivo: LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer while exhibiting no significant toxicity for mice and does not disturb the normal histology of the gut of mice.

Protocol
Cell Experiment
Cell lines The cell lines HCT116, HCT15, HT29, SW480, SW620, LS174T, SW48, MCF7, HeLa, HEK293, and MDCK
Preparation method β-catenin is immunoprecipitated from protein extracts of the cells that are incubated with LF3 at increasing concentrations, and reduced TCF4 and LEF1 bound to β-catenin are shown by Western blotting.
Concentrations 3.3-60 μmol/L
Incubation time 24 h
Animal Experiment
Animal models NOD/SCID mice
Formulation
Dosages 50 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 416.56
Formula C20H24N4O2S2
CAS Number 664969-54-4
Purity 99.91%
Solubility 63 mg/mL in DMSO
Storage at -20°C
References

[1] Fang L, et al. Cancer Res. A Small-Molecule Antagonist of the β-Catenin/TCF4 Interaction Blocks the Self-Renewal of Cancer Stem Cells and Suppresses Tumorigenesis.

[2] Xue SA, et.al. Mol Cell Biol. Genetic diversity: frameshift mechanisms alter coding of a gene (Epstein-Barr virus LF3 gene) that contains multiple 102-base-pair direct sequence repeats.

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Keywords: LF3 supplier, Wnt/beta-catenin, inhibitors

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