WNTinib

Pricing Availability   Qty
Description: Inhibitor of mutant β-catenin signaling in hepatocellular carcinoma
Chemical Name: 4-[3-Fluoro-4-[[[[4-(1,1,2,2,2-pentafluoroethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Pathways (1)

Biological Activity for WNTinib

WNTinib is a multi-kinase inhibitor with selectivity for mutant β-catenin (CTNNB1) in hepatocellular carcinoma compared to wild type hepatocytes (IC50 ranges are 0.36 μM-0.54 μM in primary organoids; 0.28 μM-1 μM in primary human HCC cell lines and 0.45 μM-2.3 μM in human cell lines ). Also inhibits VEGFR2, PDE6D and VEGFR1 (IC50 values are 0.3 μM, 0.3 μM and 0.6 μM respectively). Downregulates WNT and phospho-EZH2, upregulates trimethylation of H3K27 and normalises expression of apoptotic genes.

Technical Data for WNTinib

M. Wt 498.39
Formula C22H16F6N4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2770091-44-4
PubChem ID 170535525
InChI Key URCPDENSDRVZDE-UHFFFAOYSA-N
Smiles O=C(NC1=CC=C(C=C1F)OC2=CC(C(NC)=O)=NC=C2)NC3=CC=C(C(F)(C(F)(F)F)F)C=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for WNTinib

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.84 100

Preparing Stock Solutions for WNTinib

The following data is based on the product molecular weight 498.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.01 mL 10.03 mL 20.06 mL
5 mM 0.4 mL 2.01 mL 4.01 mL
10 mM 0.2 mL 1 mL 2.01 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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References for WNTinib

References are publications that support the biological activity of the product.

Rialdi et al (2023) WNTinib is a multi-kinase inhibitor with specificity against β-catenin mutant hepatocellular carcinoma. Nat.Cancer 4 1157 PMID: 37537299


If you know of a relevant reference for WNTinib, please let us know.

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Keywords: WNTinib, WNTinib supplier, Wnt, beta-catenin, b-catenin, catenin, CTNNB1, mutant, hepatocellular, carcinoma, kinase, inhibitor, inhibitors, Beta-catenin, 8106, Tocris Bioscience

Citations for WNTinib

Citations are publications that use Tocris products.

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Pathways for WNTinib

Wnt Signaling Pathway

Wnt Signaling Pathway

The Wnt pathway is involved in cellular differentiation and proliferation in adult tissues and also during embryogenesis. Disturbances within the pathway may lead to the formation of tumors and promote metastasis.