Defactinib (VS-6063)

Catalog No.S7654 Synonyms: PF-04554878

For research use only.

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

Defactinib (VS-6063) Chemical Structure

CAS No. 1073154-85-4

Selleck's Defactinib (VS-6063) has been cited by 35 publications

Purity & Quality Control

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 NUK4T5lHTnWwY4Tpc44h[XO|YYm= M2fFPJJm\HWlZXSgZY5lKHKndHHy[IVlKG23bITpZ4VtdHWuYYKgd5Bp\XKxaXSg[o9zdWG2aX;u MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN|MkSxNUc,Ojl|M{K0NVE9N2F-
Bel-7402 Mlz0SpVv[3Srb36gZZN{[Xl? MlfHdoVlfWOnZDDhcoQhemW2YYLk[YQhdXWudHnj[YxtfWyjcjDzdIhmem:rZDDmc5Ju[XSrb36= Moj5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl|M{K0NVEoRjJ7M{OyOFEyRC:jPh?=
PC3-mm2 M1foeWZ2dmO2aX;uJIF{e2G7 NXThO3F5XHKnYYTt[Y51KG:oIGDDN{1udTJiY3XscJMhf2m2aDDk[YZi[3SrbnniJIxm\CC2bzDhJJRqdWVvIHHu[EBld3OnLXTldIVv\GWwdDDpcohq[mm2aX;uJI9nKE[DSzDwbI9{eGixconsZZRqd25? NUHiRm9{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1N|A6ODJpPkK2OVMxQTB{PD;hQi=>
BON MVHD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MYm3NkBp M2f3cWdKPTB;NT60NkDPxE1? NHzzNno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm3NVI6Pyd-MkW5O|EzQTd:L3G+
GGP-1 Ml;UR4VtdCC4aXHibYxqfHliYYPzZZk> NGfqeWc4OiCq Mnq2S2k2OD12LkmwJO69VQ>? NEPBepo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm3NVI6Pyd-MkW5O|EzQTd:L3G+
CM M1HUNWNmdGxidnnhZoltcXS7IHHzd4F6 NEe0TJE4OiCq M4HmZWdKPTB;MT63O{DPxE1? Mn:5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7N{GyPVcoRjJ3OUexNlk4RC:jPh?=
KB-3-1 M4jk[ZFJXFNiYYPzZZk> M3r6SnAu\2y7Y3;wdo91\WmwIIP1ZpN1emG2ZYOgbYRmdnSrZnnl[EBqdiCNQj2zMVEh[WSnbn;jZZJkcW6xbXGgZ4VtdCCuaX7lMEByUFSVIITo[ZJieGW3dHnjJIxq[nKjcomgd4Nz\WWw MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTVzNUK4OEc,OzF3MUWyPFQ9N2F-
Assay
Methods Test Index PMID
Western blot HER2 pY1248 / FAK pY397 / AKT pS473 / p-ERK ; pIGF1R / IGF1R / E-cadherin / vimentin / ZEB-1 27638858 25749031
Immunofluorescence pFAK (Tyr 397) / pYB-1 (Ser 102) 24062525
Growth inhibition assay Cell viability 25971297
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 Research:[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.
  • (Only for Reference)
Animal Research:[1]
  • 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.

5mg/mL

* 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
Formula

C20H21F3N8O3S

CAS No. 1073154-85-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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