939791-39-6
Chemical Structure
PF-562271 mesylate
Synonym(s): VS-6062 mesylate
- CAS No.: 939791-39-6
- Formula:C22H24F3N7O6S2
- Molecular Weight:603.59
IUPAC Name: N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide methanesulfonate
InChIKey: LMGBAHJMBMDBFE-UHFFFAOYSA-N
SMILES: O=C1NC2=CC=C(C=C2C1)NC3=NC=C(C(=N3)NCC4=CC=CN=C4N(C)S(=O)(=O)C)C(F)(F)F.O=S(=O)(O)C
Biological Activity: PF-562271 mesylate (VS-6062 mesylate) 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 mesylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 mesylate 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 mesylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 mesylate 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].
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PF-562271 mesylate | PF-562271 mesylate (VS-6062 mesylate) 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 mesylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 mesylate 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 mesylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 mesylate 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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References
- [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]
