Defactinib
Defactinib
Defactinib
| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-4828-5MG | Defactinib | 5mg | $137.00 | |
| GBM-4828-25MG | Defactinib | 25mg | $452.00 |
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Description
Potent FAK inhibitor
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Specifications
Bioassays Specification Bio-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 Function / Pharmacology 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 in shows synergistic activity when used in combination with checkpoint immunotherapy 4-6. CAS# 1073154-85-4 MW 510.50 Molecular Formula C20H21F3N8O3S Solubility Soluble in DMSO (up to at least 25 mg/ml) Supplied powder Storage as supplied -20°C Ship temp Ambient References 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 Antibody Specification Alternate Names PF-04554878; VS-6063 Protein Specification Purity >98% - Reviews
| Bioassays Specification | |
| Bio-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 |
| Function / Pharmacology | 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 in shows synergistic activity when used in combination with checkpoint immunotherapy 4-6. |
| CAS# | 1073154-85-4 |
| MW | 510.50 |
| Molecular Formula | C20H21F3N8O3S |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 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 |
| Antibody Specification | |
| Alternate Names | PF-04554878; VS-6063 |
| Protein Specification | |
| Purity | >98% |