Pricing Availability   Qty
Description: Potent and selective FAK and Pyk2 inhibitor
Chemical Name: N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide
Purity: ≥98% (HPLC)

Biological Activity for Defactinib

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.

Compound Libraries for Defactinib

Defactinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Defactinib

M. Wt 510.49
Formula C20H21F3N8O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1073154-85-4
PubChem ID 25117126
Smiles CNC(=O)C1=CC=C(NC2=NC=C(C(NCC3=NC=CN=C3N(C)[S](C)(=O)=O)=N2)C(F)(F)F)C=C1

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 Defactinib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 51.05 100

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 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 1.96 mL 9.79 mL 19.59 mL
5 mM 0.39 mL 1.96 mL 3.92 mL
10 mM 0.2 mL 0.98 mL 1.96 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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References for Defactinib

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

Jones et al (2015) A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors. Invest. New Drugs 33 1100 PMID: 26334219

O'Brien et al (2014) FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 5 7945 PMID: 25277206

Errico et al (2021) Neurofibromin deficiency and extracellular matrix cooperate to increase transforming potential through FAK-dependent signaling. Cancers 13 PMID: 34066061

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

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Citations for Defactinib

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