Defactinib

Key Product Details

Product Description

Defactinib is a potent and selective focal adhesion kinase (FAK) and proline rich tyrosine kinase 2 (Pyk2) inhibitor (IC₅₀ = 0.6 nM at both). The compound shows >100-fold selectivity for FAK and Pyk2 over other kinases. Defactinib inhibits FAK phosphorylation in vivo (EC₅₀ = 26 nM), and inhibits tumor growth. Defactinib also decreases the viability of thyroid cancer cells, showing greater selectivity for TT and K1 cells compared to FAK Inhibitor 14 (Cat. No. 3414) (IC₅₀ values are 1.98 μM and 10.34 μM, respectively). Defactinib suppresses colony growth of Pnf cells when combined with Selumetinib (Cat. No. 6815).

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the Defactinib (PF-04554878) probe summary on the SGC website.

Product Specifications for Defactinib

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

Solubility

Preparing Stock Solutions for Defactinib

The following data is based on the product molecular weight 510.49.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.96 mL	9.79 mL	19.59 mL
5 mM	0.39 mL	1.96 mL	3.92 mL
10 mM	0.20 mL	0.98 mL	1.96 mL
50 mM	0.04 mL	0.20 mL	0.39 mL

Calculators

Background References

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

• O'Brien FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 2014 PMID: 25277206
• Errico Neurofibromin deficiency and extracellular matrix cooperate to increase transforming potential through FAK-dependent signaling. Cancers 2021 PMID: 34066061
• Jones A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors. Invest. New Drugs 2015 PMID: 26334219

Product Documents for Defactinib