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PF-562271 | FAK/Pyk2 inhibitor

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Price:
$169.00
Catalog #:
C7562-5
Quantity:


Product Description

PF-562271 is a reversible, ATP-competitive inhibitor of focal adhesion kinase (FAK) and Pyk2 with an IC50 of 1.5 and 14 nM, respectively. [1] In an inducible cell-based assay measuring phospho-FAK, it robustly inhibits at an IC50 of 5 nM. In vivo, PF-562271 inhibits FAK phosphorylation in a dose-dependent fashion at an EC50 of 93 ng/mL.

PF-562271 has been evaluated as a potential therapy for pancreatic ductal adenocarcinoma [2] and for cancer patients with bone metastases and cancer-associated osteoporosis. [3]

PF-562271 has been studied in combination with gemcitabine in pancreatic cancers, and sunitinib in hepatocellular carcinomas. [4] In the sunitinib / PF-562271 combination studies, both angiogenesis and tumor proliferation were addressed, posing a formidable approach to treating solid tumors of the liver.


Technical information:

Chemical Formula:   C21H20F3N7O3S
CAS #:   717907-75-0
Molecular Weight:   507.49
Purity:   >98%
Appearance:   White
Chemical Name:   N-methyl-N-(3-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridin-2-yl)methanesulfonamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   PF-562271, PF 562271, PF562271

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Roberts et al., Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 2008, 68, 1935-1944 Pubmed ID: 18339875
2. Stokes et al,. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol. Cancer Ther. 2011, 10, 2135-2145. Pubmed ID: 21903606
3. Bagi et al., Dual focal adhesion kinase/Pyk2 inhibitor has positive effects on bone tumors: implications for bone metastases. Cancer, 2008, 112(10), 2313-2321. Pubmed ID: 18348298
4. Bagi et al., Sunitinib and PF-562,271 (FAK/Pyk2 inhibitor) effectively block growth and recovery of human hepatocellular carcinoma in a rat xenograft model. Cancer Biol. Ther. 2009, 8(9), 856-865. Pubmed ID: 21903606

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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