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Product Details

Defactinib | Potent FAK inhibitor

Defactinib (1073154-85-4) is a potent inhibitor of FAK (IC50 = 0.6nM) and Pyk2 (IC50 = 0.6nM).1 It is active in vivo (EC50 = 26nM). FAK inhibition prevents tumor invasion and dissemination rather than tumor size reduction. Defactinib has been shown to preferentially target cancer stem cells in a mouse xenograft model of triple negative breast cancer.2 It is in multiple clinical trials for various cancers3 and it shows synergistic activity when used in combination with checkpoint immunotherapy 4-6.

References/Citations

1) 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
2) Kolev et al. (2017), Inhibition of FAK kinase activity preferentially targets cancer stem cells; Oncotarget 8 51733
3) Marcucci et al. (2016), Anti-Cancer Stem-like Cell Compounds in Clinical Development – An Overview and Critical Appraisal; Front. Oncol. 6 115
4) Ring et al. (2015), FAK/PYK2 inhibitors defactinib and VS-4718 enhance immune checkpoint inhibitor efficacy; J. Immunother. Cancer 3 354
5) NCT02546531
6) Jiang et al. (2016), 
Targeting Focal Adhesion Kinase Renders Pancreatic Cancers Responsive to Checkpoint Immunotherapy; Nat. Med. 22 851

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Catalog#  10-4828-0005

$65.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1073154-85-4
Catalog Number:
10-4828
Activity:
Potent FAK inhibitor
Chemical Name:
N-Methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]aminl]benzamide
Molecular Weight:
510.50
Molecular Formula:
C20H21F3N8O3S
Solubility:
Soluble in DMSO (up to at least 25mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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