939791-38-5
Chemical Structure
PF-562271 (besylate)
Synonym(s): VS-6062 (besylate)
- CAS No.: 939791-38-5
- Formula:C27H26F3N7O6S2
- Molecular Weight:665.66
IUPAC Name: N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide benzenesulfonate
InChIKey: LKLWTLXTOVZFAE-UHFFFAOYSA-N
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
Biological Activity: PF-562271 besylate (VS-6062 besylate) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 besylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 besylate exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 besylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 besylate can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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PF-562271 (besylate) | 99.17% | PF-562271 besylate (VS-6062 besylate) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 besylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 besylate exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 besylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 besylate can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma. | ||||||||||||||||||||
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PF-562271 besylate (Standard) | ≥98% | PF-562271 besylate (Standard) is the analytical standard of PF-562271 besylate (HY-10458). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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- [1]. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer research. 2008 Mar 15;68(6):1935-44. [Content Brief]
- [2]. Stokes JB, 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. Molecular cancer therapeutics. 2011 Nov;10(11):2135-45. [Content Brief]
- [3]. Bagi CM, 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 biology & therapy. 2009 May;8(9):856-65. [Content Brief]
