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Defactinib (VS-6063)

Name: Defactinib (VS-6063)
Brand: Selleck Chemicals
SKU: S7654
Rating: 5 (64 reviews)

Synonyms: PF-04554878

Catalog No.S7654 Purity: 99.98%

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

Defactinib (VS-6063) Chemical Structure

CAS: 1073154-85-4

Selleck's Defactinib (VS-6063) has been cited by 64 publications

Purity & Quality Control

Defactinib (VS-6063) Related Products

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Signaling Pathway

FAK Signaling Pathway

Choose Selective FAK Inhibitors

Cell Data

Cell Lines	Assay Type	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04201145	Withdrawn	Malignant Pleural Mesothelioma	Raphael Bueno MD\|Merck Sharp & Dohme LLC\|Dana-Farber Cancer Institute	September 2020	Phase 1

References

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

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.

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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