Defactinib (VS-6063, PF-04554878)

Catalog No.S7654

Defactinib (VS-6063, PF-04554878) Chemical Structure

Molecular Weight(MW): 510.49

Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

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USD 557 In stock
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Cited by 5 Publications

4 Customer Reviews

  • Immunofluorescence microscopy (1000x magnification) with p65 (red fluorescence, Cy3) revealed a cytoplasmic retention of p65 after VS-6063 treatment in HBl-2 and MINO (D).

    Haematologica, 2018, 103(1):116-125. Defactinib (VS-6063, PF-04554878) purchased from Selleck.

    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.

Purity & Quality Control

Choose Selective FAK Inhibitors

Biological Activity

Description Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Targets
FAK [1]
In vitro

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. [1] The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 NEf6SVNHfW6ldHnvckBie3OjeR?= NGTmR3Nz\WS3Y3XkJIFv\CC{ZYThdoRm\CCvdXz0bYNmdGy3bHHyJJNxcGW{b3nkJIZwem2jdHnvci=> MorkNlk{OzJ2MUG=
Bel-7402 MkjISpVv[3Srb36gZZN{[Xl? MnLRdoVlfWOnZDDhcoQhemW2YYLk[YQhdXWudHnj[YxtfWyjcjDzdIhmem:rZDDmc5Ju[XSrb36= NU\0VmtpOjl|M{K0NVE>
PC3-mm2 M1\VfGZ2dmO2aX;uJIF{e2G7 NWLRWZQ4XHKnYYTt[Y51KG:oIGDDN{1udTJiY3XscJMhf2m2aDDk[YZi[3SrbnniJIxm\CC2bzDhJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDpcohq[mm2aX;uJI9nKE[DSzDwbI9{eGixconsZZRqd25? NV74[FdTOjZ3M{C5NFI>
BON MnrxR4VtdCC4aXHibYxqfHliYYPzZZk> MVS3NkBp NF;2dmhIUTVyPUWuOFIh|ryP M3zudFI2QTdzMkm3
GGP-1 M{m2XWNmdGxidnnhZoltcXS7IHHzd4F6 MmnqO|IhcA>? NF3kdGpIUTVyPUSuPVAh|ryP M36wdlI2QTdzMkm3
CM MkLXR4VtdCC4aXHibYxqfHliYYPzZZk> MnfRO|IhcA>? NGTmR3pIUTVyPUGuO|ch|ryP MnzaNlU6PzF{OUe=

... Click to View More Cell Line Experimental Data

In vivo In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. [1]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells
  • Concentrations: ~10 μM
  • Incubation Time: 96 hours
  • Method: Ovarian cancer cells are treated with increasing concentrations of VS-6063 for 96 hours and then subjected to the MTT assay. Results are confirmed with triplicate experiments.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors
  • Formulation: PBS
  • Dosages: 50 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (9.79 mM)
Water Insoluble
Ethanol Insoluble
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.
5mg/mL

* 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.

Chemical Information

Molecular Weight 510.49
Formula

C20H21F3N8O3S

CAS No. 1073154-85-4
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03727880 Not yet recruiting Resectable Pancreatic Ductal Adenocarcinoma (PDAC)|Pancreatic Ductal Adenocarcinoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Merck Sharp & Dohme Corp.|Verastem Inc. April 2019 Phase 2
NCT03727880 Not yet recruiting Resectable Pancreatic Ductal Adenocarcinoma (PDAC)|Pancreatic Ductal Adenocarcinoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Merck Sharp & Dohme Corp.|Verastem Inc. April 2019 Phase 2
NCT02758587 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|Queen''s University Belfast July 4 2017 Phase 1|Phase 2
NCT02758587 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|Queen''s University Belfast July 4 2017 Phase 1|Phase 2
NCT02546531 Recruiting Advanced Solid Tumors|Solid Tumors|Pancreatic Cancer Washington University School of Medicine|Barnes Jewish Health Foundation|Merck Sharp & Dohme Corp.|Verastem Inc. February 3 2016 Phase 1
NCT02546531 Recruiting Advanced Solid Tumors|Solid Tumors|Pancreatic Cancer Washington University School of Medicine|Barnes Jewish Health Foundation|Merck Sharp & Dohme Corp.|Verastem Inc. February 3 2016 Phase 1

Tech Support

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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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID