Dược Lực Học :
SF1126 is a covalent conjugate of LY294002 that contains a peptide-based targeting group to help increase the localization of the drug in the neovascular component supporting tumor growth. SF1126 is a highly water soluble solid which aids its administration via i.v. or s.c. injections. In vivo it converts spontaneously at physiological pH to LY294002 in a way that is well tolerated in mice, rats, and dogs. SF1126 has been evaluated in numerous animal tumor models showing good tumor inhibition or tumor regression.
Cơ Chế Tác Dụng :
SF1126 is an integrin-targeted PI3 kinase inhibitor.
SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA isoforms and other key members of the PI3K superfamily, including DNA-PK and mTOR. A major factor in tumor resistance to approved chemotherapy agents is thought to be the activation of the PI3K/PTEN pathway. As a result, it is thought that inhibiting this pathway, via SF1126, could cause the resetting of sensitivity to approved agents and exhibit synergistic anticancer effects.
Chỉ Định :
For the treatment of various forms of cancer.