Pi3 kinase inhibitors and uses thereof

摘要

Disclosed are conjugates of one or more PI3 kinases having a cysteine residue, CysX, wherein the CysX is covalently, and irreversibly, bonded to a PI3 kinase inhibitor, wherein CysX is selected from Cys862 of PI3K-alpha, Cys2243 of MTOR, Cys838 of PI3K-alpha, Cys869 of PI3K-gamma, Cys815 of PI3K-delta, Cys841 of PI3K-beta, Class 1A, Cys 1119 of PI3K-beta, Class 2, Cys3683 of DNA-PK, Cys2770 of ATM-Kinase, Cys2753 of ATM-Kinase, Cys 1840 of PI4KA, Cys 1844 ofPI4KA, or Cysl797 of PI4KA. The compounds are PI3 Kinase inhibitors and are sometimes conjugated to a peptide sequence. In particular the kinase inhibitors are compounds of formula (II-i).