Home Angiogenesis FAK inhibitor Defactinib (VS-6063) For research use only.

Defactinib (VS-6063)

Synonyms: PF-04554878

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

Defactinib (VS-6063) Chemical Structure

Defactinib (VS-6063) Chemical Structure

CAS: 1073154-85-4

Selleck's Defactinib (VS-6063) has been cited by 66 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 Function assay reduced and retarded multicellular spheroid formation 29332411
Bel-7402 Function assay reduced and retarded multicellular spheroid formation 29332411
PC3-mm2 Function assay Treatment of PC3-mm2 cells with defactinib led to a time- and dose-dependent inhibition of FAK phosphorylation 26530902
BON Cell viability assay 72 h GI50=5.42 μM 25971297
GGP-1 Cell viability assay 72 h GI50=4.90 μM 25971297
CM Cell viability assay 72 h GI50=1.77 μM 25971297
KB-3-1 qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
Click to View More Cell Line Experimental Data

Biological Activity

Description Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
Targets
FAK [1]
In vitro
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot HER2 pY1248 / FAK pY397 / AKT pS473 / p-ERK pIGF1R / IGF1R / E-cadherin / vimentin / ZEB-1 27638858
Immunofluorescence pFAK (Tyr 397) / pYB-1 (Ser 102) 24062525
Growth inhibition assay Cell viability 25971297
In Vivo
In vivo In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. [1]
Animal Research Animal Models Mice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors
Dosages 50 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04201145 Withdrawn Malignant Pleural Mesothelioma Raphael Bueno MD|Merck Sharp & Dohme LLC|Dana-Farber Cancer Institute September 2020 Phase 1

Chemical lnformation & Solubility

Molecular Weight 510.49 Formula

C20H21F3N8O3S
CAS No. 1073154-85-4 SDF Download Defactinib (VS-6063) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (195.89 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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