Defactinib (VS-6063, PF-04554878)
Molecular Weight(MW): 510.49
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Cited by 18 Publications
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c, d MEL-JUSO cells were pre-treated with Defactinib (5 µM); e, f WM1205-LU cells were pre-treated with either inhibitor or a combination of both. Subsequently, cells were treated with trametinib (10 nM) and phosphorylation of key kinases, as well as cell viability were determined (48 h) using multiplex ELISA and resazurin reduction assay, respectively. Data show averaged median fluorescence intensity (MFI) for each protein (means ± S.D. from n = 3 independent experiments) and or cell viability relative to control values of 100% (means + S.E.M. from n = 3 independent experiments). Statistical analysis was performed using two-way ANOVA with post-hoc Tukey test
Cell Death Differ. 2018, doi: 10.1038/s41418-018-0210-8. Defactinib (VS-6063, PF-04554878) purchased from Selleck.
(C) D2.A1 cells were pretreated for 18 hours with the indicated concentration of Defactinib. (D) D2.A1 cells were pretreated for 10 minutes with indicated concentrations of Defactinib. cells were serum starved for 18 hours with or without inhibitor pretreatment and cells were subsequently stimulated with FGF2 (20ng/ml) for 30 minutes and analyzed by immunoblot for downstream phosphorylation of Erk1/2. Expression of total Erk1/2 was analyzed as a loading control.
Mol Cancer Ther, 2016, 15(9):2096-106. Defactinib (VS-6063, PF-04554878) purchased from Selleck.
Western blot analysis of phosphorylated FAK Y397 levels in SCC42B and FaDu cells treated with increasing concentrations of the FAK inhibitors PF-573228, PF-562271 and VS-6063 for 1 h. GAPDH levels were used as loading control.
Cancer Epidemiology, 2018, doi:10.1158/1055-9965.EPI-17-1082. Defactinib (VS-6063, PF-04554878) purchased from Selleck.
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Choose Selective FAK Inhibitors
|Description||Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.|
In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, VS-6063 significantly inhibits pFAK (Tyr397) expression. The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells.  The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines. 
|In vivo||In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. |
|In vitro||DMSO||5 mg/mL warmed (9.79 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02943317||Terminated||Drug: Part A - VS-6063|Drug: Part A - Avelumab||Epithelial Ovarian Cancer||Verastem Inc.||October 2016||Phase 1|
|NCT02004028||Recruiting||Drug: VS-6063||Malignant Pleural Mesothelioma||Verastem Inc.||December 2013||Phase 2|
|NCT01943292||Completed||Drug: Defactinib||Non Hematologic Cancers||Verastem Inc.||September 2 2013||Phase 1|
|NCT01870609||Terminated||Drug: defactinib (VS-6063)|Drug: Placebo||Malignant Pleural Mesothelioma||Verastem Inc.||September 2013||Phase 2|
|NCT01951690||Completed||Drug: defactinib (VS-6063)||Non Small Cell Lung Cancer|Lung Cancer||Verastem Inc.||September 2013||Phase 2|
|NCT01778803||Completed||Drug: defactinib|Drug: Paclitaxel||Ovarian Cancer||Verastem Inc.||February 26 2013||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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