PF-562271 besylate (Synonyms: VS-6062 besylate)

Name: PF-562271 besylate
Brand: MedChemExpress
SKU: HY-10458
Rating: 5.0 (24 reviews)

Cat. No.: HY-10458 Purity: 99.17%: FAQs
Data Sheet SDS COA Handling Instructions

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PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC₅₀ of 1.5 nM and 13 nM, respectively.

For research use only. We do not sell to patients.

PF-562271 besylate Chemical Structure

CAS No. : 939791-38-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 232	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 232	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 24 publication(s) in Google Scholar

Other Forms of PF-562271 besylate:

PF-562271 In-stock
PF-562271 hydrochloride Get quote

20 Publications Citing Use of MCE PF-562271 besylate

: PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 24;14(2):157. [Abstract]; PF-562271 (250 nM; 6 h) largely inhibits Akt-S6 phosphorylation in OE-MXRA5 priPC-1 cells.

: PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59. [Abstract]; 786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.

: PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Practical Oncology Journal. 2015, 29(5): 444-449.; Effects and mechanism of Biglycan and FAK signaling pathway on the invasion and metastasis of colon cancer cells.

: PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83. [Abstract]; FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.

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Description

PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC₅₀ of 1.5 nM and 13 nM, respectively^[1].

IC₅₀ & Target

IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	2.1 μM Compound: PF-562271	Antiproliferative activity against human A549 cells after 2 days by spectrophotometric analysis Antiproliferative activity against human A549 cells after 2 days by spectrophotometric analysis	[PMID: 30340900]
HeLa	GI₅₀	1.7 μM Compound: PF-562271	Antiproliferative activity against human HeLa cells after 2 days by spectrophotometric analysis Antiproliferative activity against human HeLa cells after 2 days by spectrophotometric analysis	[PMID: 30340900]
HepG2	GI₅₀	1.2 μM Compound: PF-562271	Antiproliferative activity against human HepG2 cells after 2 days by spectrophotometric analysis Antiproliferative activity against human HepG2 cells after 2 days by spectrophotometric analysis	[PMID: 30340900]
OVCAR-3	GI₅₀	1.8 μM Compound: PF-562271	Antiproliferative activity against human OVCAR3 cells after 2 days by spectrophotometric analysis Antiproliferative activity against human OVCAR3 cells after 2 days by spectrophotometric analysis	[PMID: 30340900]
U-87MG ATCC	GI₅₀	3.7 μM Compound: PF-562271	Antiproliferative activity against human U87MG cells after 2 days by spectrophotometric analysis Antiproliferative activity against human U87MG cells after 2 days by spectrophotometric analysis	[PMID: 30340900]

In Vitro

PF-562271 (VS-6062) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays^[1]. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays^[2]. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC₅₀ of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3^[1]. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

665.66

Formula

C₂₇H₂₆F₃N₇O₆S₂

CAS No.

939791-38-5

Appearance

Solid

Color

Off-white to light yellow

SMILES

CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.O=S(C5=CC=CC=C5)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 21.4 mg/mL (32.15 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5023 mL	7.5113 mL	15.0227 mL
5 mM	0.3005 mL	1.5023 mL	3.0045 mL
10 mM	0.1502 mL	0.7511 mL	1.5023 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.17%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (254 KB) HNMR (209 KB) LCMS (252 KB)

Handling Instructions (2659 KB)

References

[1]. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944. [Content Brief]

[2]. Lim ST, et al. FERM control of FAK function: implications for cancer therapy. Cell Cycle, 2008, 7(15), 2306-2314. [Content Brief]

[3]. Canel M, et al. Quantitative in vivo imaging of the effects of inhibiting integrin signaling via Src and FAK on cancer cell movement: effects on E-cadherin dynamics. Cancer Res, 2010, 70(22), 9413-9422. [Content Brief]

Kinase Assay ^[1]	Briefly, purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl₂] for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2mol/LH₂SO₄). IC₅₀ values are determined using the Hill-Slope Model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×10⁶ cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of appr 150 mm³ in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm³) is measured with Vernier calipers and calculated. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944. [Content Brief] [2]. Lim ST, et al. FERM control of FAK function: implications for cancer therapy. Cell Cycle, 2008, 7(15), 2306-2314. [Content Brief] [3]. Canel M, et al. Quantitative in vivo imaging of the effects of inhibiting integrin signaling via Src and FAK on cancer cell movement: effects on E-cadherin dynamics. Cancer Res, 2010, 70(22), 9413-9422. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5023 mL	7.5113 mL	15.0227 mL	37.5567 mL
	5 mM	0.3005 mL	1.5023 mL	3.0045 mL	7.5113 mL
	10 mM	0.1502 mL	0.7511 mL	1.5023 mL	3.7557 mL
	15 mM	0.1002 mL	0.5008 mL	1.0015 mL	2.5038 mL
	20 mM	0.0751 mL	0.3756 mL	0.7511 mL	1.8778 mL
	25 mM	0.0601 mL	0.3005 mL	0.6009 mL	1.5023 mL
	30 mM	0.0501 mL	0.2504 mL	0.5008 mL	1.2519 mL

PF-562271 besylate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-562271 besylate939791-38-5VS-6062 besylateFAKPyk2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2Inhibitorinhibitorinhibit

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PF-562271 besylate (Synonyms: VS-6062 besylate)

Customer Review

Other Forms of PF-562271 besylate:

PF-562271 besylate Related Antibodies

20 Publications Citing Use of MCE PF-562271 besylate

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References

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Complete Stock Solution Preparation Table

PF-562271 besylate Related Classifications

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