Defactinib | Potent FAK inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $65.00 | ||
| 25 mg | $215.00 |
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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
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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1-855-FOCUS21
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