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PF-562271

Catalog No. T2465 CAS 717907-75-0

Synonyms: PF 562271, PF562271

PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).

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PF-562271, CAS 717907-75-0

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Purity: 98%

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Description	PF-562271 is an effective ATP-competitive, reversible inhibitor of FAK(IC50=1.5 nM) and Pyk2 kinase(IC50=13 nM).
Targets&IC50	PYK2:13 nM, FAK:1.5 nM
Kinase Assay	The 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 (2 M H2SO4). IC50 values are determined using the Hill-Slope Model[1].
Cell Research	PF-562271 (Haoyuan Chemexpress Co., Ltd.) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or Dasatinib. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×103 Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC50 values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×103 cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction[2].

Synonyms	PF 562271, PF562271
Molecular Weight	507.49
Formula	C21H20F3N7O3S
CAS No.	717907-75-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 93 mg/mL (183.3 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Roberts WG, et al. Cancer Res, 2008, 68(6), 1935-1944. 2. Lim ST, et al. Cell Cycle, 2008, 7(15), 2306-2314. 3. Canel M, et al. Cancer Res, 2010, 70(22), 9413-9422. 4. Sun H, et al. Cancer Biol Ther, 2010, 10(1), 38-43. 5. Bagi CM, et al. Cancer, 2008, 112(10), 2313-2321.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Cardiovascular Disease Compound Library Inhibitor Library Cell Cycle Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Cytoskeletal Signaling Pathway Compound Library

Related Products

Related compounds with same targets

PF-562271 besylate PF-562271 PF-431396 PF-562271 hydrochloride NVP-TAE 226 AZ7550

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-562271 717907-75-0 蛋白酪氨酸激酶细胞骨架细胞周期血管生成 PYK2 CDK FAK Cancer PTK2 Ewing Antitumor Pyk2 PTK2 protein tyrosine kinase 2 Sarcoma PF562271 inhibit PF 562271 Breast Focal adhesion kinase VS 6062 VS6062 Inhibitor Proline-rich tyrosine kinase 2 VS-6062 inhibitor

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