Defactinib (VS-6063)

Catalog No.S7654 Batch:S765407

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Technical Data

Formula

C20H21F3N8O3S
Molecular Weight 510.49 CAS No. 1073154-85-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (195.89 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 50%PEG300 5%Tween80 40%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (9.79mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 500 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 400 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]
In vivo

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

Protocol (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    Mice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors

  • Dosages

    50 mg/kg

  • Administration

    p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/24062525/
  • https://pubmed.ncbi.nlm.nih.gov/25277206/

Customer Product Validation

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).

Data from [ , , Haematologica, 2018, 103(1):116-125 ]

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

Data from [ , , Cell Death Differ. 2018, doi: 10.1038/s41418-018-0210-8 ]

(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.

Data from [ , , Mol Cancer Ther, 2016, 15(9):2096-106 ]

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.

Data from [ , , Cancer Epidemiology, 2018, doi:10.1158/1055-9965.EPI-17-1082 ]

Selleck's Defactinib (VS-6063) has been cited by 84 publications

Epstein-Barr virus induces aberrant B cell migration and diapedesis via FAK-dependent chemotaxis pathways [ Nat Commun, 2025, 16(1):4581] PubMed: 40389409
Role of the androgen receptor in melanoma aggressiveness [ Cell Death Dis, 2025, 16(1):34] PubMed: 39837817
DIRAS3 Inhibits Ovarian Cancer Cell Growth by Blocking the Fibronectin-Mediated Integrin β1/FAK/AKT Signaling Pathway [ Cells, 2025, 14(16)1250] PubMed: 40862729
Therapeutic benefit of the dual ALK/FAK inhibitor ESK440 in ALK-driven neuroblastoma [ Neoplasia, 2025, 60:100964] PubMed: 39900433
The role of focal adhesion kinase in bladder cancer: translation from in vitro to ex vivo human urothelial carcinomas [ Radiol Oncol, 2025, 59(3):349-367] PubMed: 40959921
A novel DNA repair protein, N-Myc downstream regulated gene 1 (NDRG1), links stromal tumour microenvironment to chemoresistance [ bioRxiv, 2025, 2025.01.22.634323] PubMed: 39896456
FAK Drives Resistance to Therapy in HPV-Negative Head and Neck Cancer in a p53-Dependent Manner [ Clin Cancer Res, 2024, 30(1):187-197] PubMed: 37819945
SPHK1 promotes bladder cancer metastasis via PD-L2/c-Src/FAK signaling cascade [ Cell Death Dis, 2024, 15(9):678] PubMed: 39284838
Tumor microenvironment-induced FOXM1 regulates ovarian cancer stemness [ Cell Death Dis, 2024, 15(5):370] PubMed: 38806454
ALK upregulates POSTN and WNT signaling to drive neuroblastoma [ Cell Rep, 2024, 43(3):113927] PubMed: 38451815

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.