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VS-4718 (PND-1186) FAK inhibitor

Cat.No.S7653

VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM, which selectively promotes tumor cell apoptosis. Phase 1.

VS-4718 (PND-1186) FAK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 501.5

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	EGFR VEGFR JAK FGFR PDGFR Src HIF HER2 FLT3 FLT
Other FAK Inhibitors	Defactinib (VS-6063) PF-562271 (VS-6062) PF-573228 PF-562271 HCl PF-562271 Besylate TAE226 (NVP-TAE226) GSK2256098 PF-431396 Y15 Ifebemtinib (IN10018, BI-853520)

Q&A of VS-4718 (PND-1186): Insights Rooted in Extensive Publications, Every Answer Cited

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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 100 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 100 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.25mg/ml (0.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.25mg/ml (0.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

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.

Read more about VS-4718 (PND-1186) solubility in DMSO or water

Search directly for a cell line, or select a cell line to find matched working concentrations

Read more about VS-4718 (PND-1186) working concentrations for cell culture treatment

VS-4718 (PND-1186) is a potent inhibitor of FAK (21870 nM), PYK2, FLT3. VS-4718 (PND-1186) exhibits the greatest inhibitory potency toward FAK (IC50 = 21870 nM).

Read more about selectivity & specificity

Mechanism of Action

Information	VS-4718 (PND-1186) is a potent, selective, and reversible ATP-competitive FAK inhibitor. It affects FAK/Src and PI3K/Akt signaling, by binding to the kinase domain and blocking FAK autophosphorylation at Tyr397, inhibiting tumor cell proliferation, migration, and invasion.
Read more about VS-4718 (PND-1186) IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about VS-4718 (PND-1186) Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	501.5	Formula	C₂₅H₂₆F₃N₅O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1061353-68-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SR-2156			Smiles	CNC(=O)C1=CC=CC=C1NC2=CC(=NC=C2C(F)(F)F)NC3=C(C=C(C=C3)N4CCOCC4)OC

Read more about storage & stability

Read more comparative analysis about VS-4718 (PND-1186)

Tech Support

Handling Instructions

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

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

Frequently Asked Questions

Question 1:
Whether the in vivo formulation of this compound using 2% DMSO+30% PEG 300+5% Tween 80+ddH2O is suitable for injection?

Answer:
A clear solution with the highest concentration at 5 mg/ml can be generated using the formulation: 2% DMSO + 30% PEG 300 + 5% Tween 80 + ddH₂O. It may be suitable for oral administration or injection.

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 )

*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

Concentration (start):

Dilution-folds:

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):