Defactinib
Tocris Bioscience, part of Bio-Techne | Catalog # 7305
Potent and selective FAK and Pyk2 inhibitor
Key Product Details
Description
Potent and selective FAK and Pyk2 inhibitor
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
Molecular Weight
510.49
Formula
C20H21F3N8O3S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide
CAS Number
1073154-85-4
PubChem ID
25117126
InChI Key
FWLMVFUGMHIOAA-UHFFFAOYSA-N
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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 all affect the solvent volumes required to prepare stock solutions.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for Defactinib
For research use only
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