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    Defactinib (VS6063, PF04554878)
    Defactinib (VS6063, PF04554878)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0663
    CAS #: 1073154-85-4 Purity ≥98%

    Description: Defactinib (formerly known as VS-6063, PF-04554878) is a selective, ATP-competitive and orally bioactive small molecule inhibitor of the FAK (focal adhesion kinase) with potential antitumor activity. It inhibits the phosphorylation of FAK at the Tyr397 site in a time- and dose-dependent manner. FAK is a nonreceptor tyrosine kinase that plays a vital role in many oncogenic pathways. Increased FAK expression has been reported in a number of tumor types, including breast, colon, and ovarian cancers. Therefore, as an inhibitor of FAK, defactinib has potential antineoplastic activities. 

    References: J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95; Oncotarget. 2014 Sep 15;5(17):7945-59.

    Related CAS: 1073154-85-4 (free base); 1345713-71-4 (free base); 1073160-26-5 (HCl)

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    Molecular Weight (MW)510.49
    FormulaC20H21F3N8O3S
    CAS No.1073154-85-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (9.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+50% PEG 300+5% Tween 80+ddH2O: 5mg/mL 
    SynonymsVS-6063; PF-04554878; VS6063; VS 6063; PF04554878; PF 04554878; PF4554878;  

    Chemical Name: N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide

    SMILES Code: O=C(NC)C1=CC=C(NC2=NC=C(C(F)(F)F)C(NCC3=NC=CN=C3N(C)S(=O)(C)=O)=N2)C=C1


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    In Vitro

    In vitro activity: In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, Defactinib significantly inhibits pFAK (Tyr397) expression. The combination of Defactinib and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. The combination of Defactinib and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines.


    Kinase Assay: Defactinib inhibited FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. The combination of Defactinib and paclitaxel markedly decreased proliferation and increased apoptosis, which resulted in 92.7% to 97.9% reductions in tumor weight. RPPA data showed that Defactinib reduced levels of AKT and YB-1 in taxane-resistant cell lines. FAK inhibition enhanced chemosensitivity in taxane-resistant cells by decreasing YB-1 phosphorylation and subsequently CD44 in an AKT-dependent manner. In human ovarian cancer samples, nuclear FAK expression was associated with increased nuclear YB-1 expression (χ²) = 37.7; P < .001). Coexpression of nuclear FAK and YB-1 was associated with statistically significantly worse median overall survival (24.9 vs 67.3 months; hazard ratio = 2.64; 95% confidence interval = 1.38 to 5.05; P = .006).


    Cell Assay: Ovarian cancer cells are treated with increasing concentrations of Defactinib for 96 hours and then subjected to the MTT assay. Results are confirmed with triplicate experiments.

    In VivoIn both PTX-sensitive and PTX-resistant models, Defactinib (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel.
    Animal modelMice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors
    Formulation & DosageDissolved in PBS; 50 mg/kg; Administered through p.o. 
    ReferencesJ Natl Cancer Inst. 2013 Oct 2;105(19):1485-95; Oncotarget. 2014 Sep 15;5(17):7945-59.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Defactinib (PF-04554878)

    Y15 and PF-04554878 decreased cell viability in a dose-dependent manner in thyroid cancer cell lines. Oncotarget. 2014 Sep 15;5(17):7945-59.

    Defactinib (PF-04554878)

    Y15 and PF-04554878 induced significant gene changes in medullary thyroid cancer TT cells. Oncotarget. 2014 Sep 15;5(17):7945-59.

    Defactinib (PF-04554878)

    Y15 and PF-04554878 decreased clonogenicity in a dose-dependent manner in papillary thyroid cancer cell lines. Oncotarget. 2014 Sep 15;5(17):7945-59.

    Defactinib (PF-04554878)

    In vitro biological effects of VS-6063 on taxane-sensitive and taxane-resistant cell lines.  2013 Oct 2;105(19):1485-95.

    Defactinib (PF-04554878)

    In vivo effects of VS-6063 combined with paclitaxel (PTX).  2013 Oct 2;105(19):1485-95.

    Defactinib (PF-04554878)

    VS-6063 restores YB-1–mediated paclitaxel (PTX) resistance.  2013 Oct 2;105(19):1485-95.

    Defactinib (PF-04554878)

    VS-6063 downregulated YB-1 phosphorylation and nuclear translocation in taxane-resistant cells by an AKT-dependent pathway.  2013 Oct 2;105(19):1485-95.




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