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.
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(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.
Purity & Quality Control
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 individually and in order:
5% DMSO+50% PEG 300+5% Tween 80+ddH2O
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02758587||Not yet recruiting||Carcinoma, Non-small-cell Lung|Mesothelioma|Pancreatic Neoplasms||NHS Greater Glasgow and Clyde|University of Glasgow|Cancer Research UK|Merck Sharp & Dohme Corp.|Verastem, Inc.|University of Edinburgh|University of Southampton|University of Leicester|Queens University, Belfast||June 2016||Phase 1|Phase 2|
|NCT02546531||Recruiting||Advanced Solid Tumors|Solid Tumors|Pancreatic Cancer||Washington University School of Medicine||January 2016||Phase 1|
|NCT02913716||Completed||Healthy Subjects||Verastem, Inc.||August 2015||Phase 1|
|NCT02465060||Recruiting||Advanced Malignant Neoplasm|Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Solid Neoplasm|Refractory Malignant Neoplasm|Refractory Plasma Cell Myeloma||National Cancer Institute (NCI)||August 2015||Phase 2|
|NCT01943292||Completed||Non Hematologic Cancers||Verastem, Inc.||September 2013||Phase 1|
|NCT01870609||Terminated||Malignant Pleural Mesothelioma||Verastem, Inc.||September 2013||Phase 2|
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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