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.
