Defactinib (VS-6063)

For research use only.

Catalog No.S7654 Synonyms: PF-04554878

34 publications

Defactinib (VS-6063) Chemical Structure

CAS No. 1073154-85-4

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

Selleck's Defactinib (VS-6063) has been cited by 34 publications

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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 NUHse4V{TnWwY4Tpc44h[XO|YYm= Mm\6doVlfWOnZDDhcoQhemW2YYLk[YQhdXWudHnj[YxtfWyjcjDzdIhmem:rZDDmc5Ju[XSrb36= NGflVJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUOzNlQyOSd-MkmzN|I1OTF:L3G+
Bel-7402 MVHGeY5kfGmxbjDhd5NigQ>? NISxZW5z\WS3Y3XkJIFv\CC{ZYThdoRm\CCvdXz0bYNmdGy3bHHyJJNxcGW{b3nkJIZwem2jdHnvci=> MoX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl|M{K0NVEoRjJ7M{OyOFEyRC:jPh?=
PC3-mm2 MlH0SpVv[3Srb36gZZN{[Xl? NH\VV3FVemWjdH3lcpQhd2ZiUFOzMY1uOiClZXzsd{B4cXSqIHTl[oFkfGmwaXKgcIVlKHSxIHGgeIlu\S1iYX7kJIRwe2VvZHXw[Y5l\W62IHnubIljcXSrb36gc4YhTkGNIIDoc5NxcG:{eXzheIlwdg>? M2jnRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUOwPVAzLz5{NkWzNFkxOjxxYU6=
BON MWnD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MUO3NkBp NULsTFJTT0l3ME21MlQzKM7:TR?= NVPtcWU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|EzQTdpPkK1PVcyOjl5PD;hQi=>
GGP-1 M2PTWmNmdGxidnnhZoltcXS7IHHzd4F6 MWq3NkBp M1Tnd2dKPTB;ND65NEDPxE1? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl5MUK5O{c,OjV7N{GyPVc9N2F-
CM NYi5R3ZMS2WubDD2bYFjcWyrdImgZZN{[Xl? NFfNNGk4OiCq NYToWo9[T0l3ME2xMlc4KM7:TR?= MoPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7N{GyPVcoRjJ3OUexNlk4RC:jPh?=
KB-3-1 MUfxTHRUKGG|c3H5 NH;ZW4hRNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtN{0yKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbh?= M2XiOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=

... 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
  • 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 PF-04554878
Smiles CNC(=O)C1=CC=C(C=C1)NC2=NC=C(C(=N2)NCC3=NC=CN=C3N(C)S(=O)(=O)C)C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04625270 Recruiting Drug: VS-6766|Drug: VS-6766 and Defactinib Ovarian Cancer Verastem Inc.|European Network of Gynaecological Oncological Trial Groups (ENGOT)|GOG Foundation December 21 2020 Phase 2
NCT04620330 Recruiting Drug: VS-6766|Drug: VS-6766 and Defactinib Non Small Cell Lung Cancer|KRAS Activating Mutation Verastem Inc. December 31 2020 Phase 2
NCT04201145 Withdrawn Drug: Pembrolizumab|Drug: Defactinib Malignant Pleural Mesothelioma Raphael Bueno MD|Merck Sharp & Dohme Corp.|Dana-Farber Cancer Institute September 2020 Phase 1
NCT02943317 Terminated Drug: Part A - VS-6063|Drug: Part A - Avelumab Epithelial Ovarian Cancer Verastem Inc. October 2016 Phase 1
NCT02004028 Terminated Drug: VS-6063 Malignant Pleural Mesothelioma Verastem Inc. December 12 2013 Phase 2
NCT01943292 Completed Drug: Defactinib Non Hematologic Cancers Verastem Inc. September 2 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