In vitro
MP470 exhibits low microM IC50 in prostate cancer cell lines. MP470 in combination with Erlotinib shows additive effects on both cytotoxicity and induction of apoptosis. MP470 reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. MP470 was shown to inhibit dsDNA break repair and increase apoptosis. MP470 influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK3beta. Amuvatinib shows in vitro inhibitory activity against multiple human tyrosine kinases including mutant KIT and PDGFRalpha. Amuvaninib inhibited RAD51 protein expression and HR, which is associated with reduced ribosomal protein S6 phosphorylation and inhibition of global translation. Amuvatinib can sensitize cells to IR and MMC, agents that are selectively toxic to HR-deficient cells.
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