Defactinib (VS-6063)

For research use only.

Catalog No.S7654 Synonyms: PF-04554878

28 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.

Size Price Stock Quantity  
USD 107 In stock
USD 297 In stock
USD 557 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Defactinib (VS-6063) has been cited by 28 publications

Purity & Quality Control

Choose Selective FAK Inhibitors

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 NHzOXHpHfW6ldHnvckBie3OjeR?= NV;ZfYN7emWmdXPl[EBidmRicnX0ZZJl\WRibYXseIlk\WyudXzhdkB{eGincn;p[EBnd3KvYYTpc44> M2i5SFI6OzN{NEGx
Bel-7402 MnXkSpVv[3Srb36gZZN{[Xl? M{fyfZJm\HWlZXSgZY5lKHKndHHy[IVlKG23bITpZ4VtdHWuYYKgd5Bp\XKxaXSg[o9zdWG2aX;u MknBNlk{OzJ2MUG=
PC3-mm2 NGfxdYJHfW6ldHnvckBie3OjeR?= MUDUdoVifG2nboSgc4YhWEN|LX3tNkBk\WyuczD3bZRpKGSnZnHjeIlvcWJibHXkJJRwKGFidHnt[U0h[W6mIHTvd4Uu\GWyZX7k[Y51KGmwaHnibZRqd25ib3[gSmFMKHCqb4PwbI9zgWyjdHnvci=> NHHnXJAzPjV|MEmwNi=>
BON MYnD[YxtKH[rYXLpcIl1gSCjc4PhfS=> Mn;ZO|IhcA>? M1\JWmdKPTB;NT60NkDPxE1? M37QWVI2QTdzMkm3
GGP-1 MV7D[YxtKH[rYXLpcIl1gSCjc4PhfS=> NV\6do41PzJiaB?= M{P3NGdKPTB;ND65NEDPxE1? MUiyOVk4OTJ7Nx?=
CM NFrWfm9E\WyuII\pZYJqdGm2eTDhd5NigQ>? NIraNnM4OiCq M1fx[GdKPTB;MT63O{DPxE1? MlvQNlU6PzF{OUe=

... Click to View More Cell Line Experimental Data

Assay
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
Immunofluorescence
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. 

24062525
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. 

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

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.
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 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04201145 Not yet recruiting 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
NCT01870609 Terminated Drug: defactinib (VS-6063)|Drug: Placebo Malignant Pleural Mesothelioma Verastem Inc. September 2013 Phase 2
NCT01951690 Completed Drug: defactinib (VS-6063) Non Small Cell Lung Cancer|Lung Cancer Verastem Inc. September 2013 Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

FAK Signaling Pathway Map

Related FAK Products

Tags: buy Defactinib|Defactinib ic50|Defactinib price|Defactinib cost|Defactinib solubility dmso|Defactinib purchase|Defactinib manufacturer|Defactinib research buy|Defactinib order|Defactinib mouse|Defactinib chemical structure|Defactinib mw|Defactinib molecular weight|Defactinib datasheet|Defactinib supplier|Defactinib in vitro|Defactinib cell line|Defactinib concentration|Defactinib nmr|Defactinib in vivo|Defactinib clinical trial|Defactinib inhibitor|Defactinib Angiogenesis inhibitor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID