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> PF-562271 [717907-75-0]

PF-562271 [717907-75-0]

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Référence HY-10459-5mg

Conditionnement : 5mg

Marque : MedChemExpress


Description

PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s 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
A375P GI50
10.22 μM
Compound: PF-562271
Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
[PMID: 34324343]
HCT-116 GI50
1.14 μM
Compound: PF-562271
Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
[PMID: 34324343]
MDA-MB-231 GI50
1.95 μM
Compound: PF-562271
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
[PMID: 34324343]
Sf21 IC50
13 nM
Compound: PF562271
Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells
Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells
[PMID: 27876318]
Sf9 IC50
1.5 nM
Compound: PF562271
Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP
Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP
[PMID: 27876318]
SMMC-7721 IC50
23.92 μM
Compound: PF-562271
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
[PMID: 34214842]
In Vitro

PF-562271 (VS-6062) is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC50 of 5 nM[1].
PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC50 of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC50 concentrations of 2.1 and 1.7 μM, respectively[2].

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

PF-562271 Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 66.67 mg/mL (131.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9705 mL 9.8524 mL 19.7048 mL
5 mM 0.3941 mL 1.9705 mL 3.9410 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 (3.29 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% Corn Oil

    Solubility: ≥ 1.67 mg/mL (3.29 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.
Pureté et documentation
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