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 297 In stock
USD 557 In stock
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Cited by 18 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.
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 M3\rdmZ2dmO2aX;uJIF{e2G7 MXHy[YR2[2WmIHHu[EBz\XSjcnTl[EBufWy2aXPlcIx2dGG{IIPwbIVzd2mmIH\vdo1ifGmxbh?= MWGyPVM{OjRzMR?=
Bel-7402 MUXGeY5kfGmxbjDhd5NigQ>? NWewVZdHemWmdXPl[EBidmRicnX0ZZJl\WRibYXseIlk\WyudXzhdkB{eGincn;p[EBnd3KvYYTpc44> MYOyPVM{OjRzMR?=
PC3-mm2 NFfwW5ZHfW6ldHnvckBie3OjeR?= M2fLdXRz\WG2bXXueEBw\iCSQ{OtcY0zKGOnbHzzJJdqfGhiZHXmZYN1cW6rYjDs[YQhfG9iYTD0bY1mNSCjbnSg[I9{\S2mZYDlcoRmdnRiaX7obYJqfGmxbjDv[kBHSUticHjvd5Bpd3K7bHH0bY9v NFe2eI0zPjV|MEmwNi=>
BON NYfSZodjS2WubDD2bYFjcWyrdImgZZN{[Xl? MU[3NkBp MkHxS2k2OD13LkSyJO69VQ>? NIHLRmwzPTl5MUK5Oy=>
GGP-1 NEDS[XdE\WyuII\pZYJqdGm2eTDhd5NigQ>? NIWxZoQ4OiCq NUC5bXhrT0l3ME20MlkxKM7:TR?= M2rINFI2QTdzMkm3
CM NHX6cm9E\WyuII\pZYJqdGm2eTDhd5NigQ>? NYj2U2tRPzJiaB?= M1\FbmdKPTB;MT63O{DPxE1? MkPYNlU6PzF{OUe=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
HER2 pY1248 / FAK pY397 / AKT pS473 / p-ERK; 

PubMed: 27638858     

Immunoblots showing phosphorylation of FAK and downstream molecules in HER2+ breast cancer cells MDA-MB-453. Cancer cells were serum-starved overnight followed by drug treatment with FAK-kinase inhibitor (defactinib, PF-228, PF-271) or HER2/EGFR inhibitor (Lapatinib) for 1 hour and stimulated with either Heregulin-β1 (HRG) or 30 min. Images shown are representative of three independent experiments. 

pIGF1R / IGF1R / E-cadherin / vimentin / ZEB-1 ; 

PubMed: 25749031     

Total protein lysates from (C) MDA-MB-231 treated with vehicle control (DMSO), 0.5 μM PF228 or 0.5 μM PF878 for various time points (0, 30’, 1 h, 3 h, and 24 h) were analyzed via Western blotting for expression of pFAK, FAK, pIGF1R, IGF1R, E-cadherin, vimentin, and ZEB-1. β-actin served as a loading control.

27638858 25749031
pFAK (Tyr 397) / pYB-1 (Ser 102); 

PubMed: 24062525     

Immunofluorescence staining of pFAK (Tyr 397) and pYB-1 (Ser 102) of HeyA8-MDR cells treated with VS-6063 and/or PTX (at the median inhibitory concentration levels for HeyA8) for 48 hours. 

Growth inhibition assay
Cell viability; 

PubMed: 25971297     

Viability of BON, QGP-1, and CM cells treated for 72 hours with increasing doses of PF-04554878 as determined by MTT assay. Percent viability was calculated by normalizing absorbance to DMSO control. Error bars represent standard deviation of the mean. 

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


Cell Research:[1]
- Collapse
  • 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]
- Collapse
  • 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.

* 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


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

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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

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FAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID