Defactinib

Pricing Availability   Qty
Cat.No. 7305 - Defactinib | C20H21F3N8O3S | CAS No. 1073154-85-4
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)
Datasheet
Citations
Reviews
Literature (2)

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.

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
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.

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

Solubility Data for Defactinib

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 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.

View Related Products by Product Action

View all Focal Adhesion Kinase Inhibitors

Keywords: Defactinib, Defactinib supplier, vs6063, PF04554878, potent, selective, inhibitors, focal, adhesion, kinases, FAK, Pyk2, SGC, PTK, PTK2B, Focal, Adhesion, Kinase, 7305, Tocris Bioscience

Citations for Defactinib

Citations are publications that use Tocris products.

Currently there are no citations for Defactinib. Do you know of a great paper that uses Defactinib from Tocris? Please let us know.

Reviews for Defactinib

There are currently no reviews for this product. Be the first to review Defactinib and earn rewards!

Have you used Defactinib?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases