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)
Clear solution
5%DMSO 50%PEG300 5%Tween80 40%ddH2O
5.0mg/ml 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 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]
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 (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.

Customer Product Validation

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

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

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

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

Selleck's Defactinib (VS-6063) has been cited by 68 publications

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
ALK upregulates POSTN and WNT signaling to drive neuroblastoma [ Cell Rep, 2024, 43(3):113927] PubMed: 38451815
Phosphoproteomic Analysis Identified Mutual Phosphorylation of FAK and Src as a Mechanism of Osimertinib Resistance in EGFR-Mutant Lung Cancer [ JTO Clin Res Rep, 2024, 5(4):100668] PubMed: 38646155
Histone deacetylase inhibitors promote breast cancer metastasis by elevating NEDD9 expression [ Signal Transduct Target Ther, 2023, 8(1):11] PubMed: 36604412
FAK suppresses antigen processing and presentation to promote immune evasion in pancreatic cancer [ Gut, 2023, gutjnl-2022-327927] PubMed: 36977556
FAK suppresses antigen processing and presentation to promote immune evasion in pancreatic cancer [ Gut, 2023, 1–2] PubMed: None
Epigenetic suppression of PGC1α (PPARGC1A) causes collateral sensitivity to HMGCR-inhibitors within BRAF-treatment resistant melanomas [ Nat Commun, 2023, 14(1):3251] PubMed: 37277330
GSNOR deficiency promotes tumor growth via FAK1 S-nitrosylation [ Cell Rep, 2023, 42(1):111997] PubMed: 36656716
FAK-mediated phosphorylation at Y464 regulates p85β nuclear translocation to promote tumorigenesis of ccRCC by repressing RB1 expression [ Cell Rep, 2023, 42(3):112188] PubMed: 36857183
FTO facilitates cancer metastasis by modifying the m6A level of FAP to induce integrin/FAK signaling in non-small cell lung cancer [ Cell Commun Signal, 2023, 10.1186/s12964-023-01343-6] PubMed: 37919739

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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.