VVD-844 is an orally active covalent inhibitor of PI3Kα , which inhibits Pl3Kα/p110α interaction with an IC 50 of 4 nM. VVD-844 covalently binds to Cys 242 in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2 -overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers.
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