INCB3619 (INCB-3619) is a potent, selective and orally active ADAM10/17 inhibitor with IC50 of 22 nM and 14 nM for ADAM10 and ADAM17, respectively.
INCB3619 has some MMP2 and MMP12 inhibitory activities.
INCB3619 inhibits heregulin cleavage with an IC50 value of 0.24 uM, INCB3619 can prevent the cleavage of TGFα, HB-EGF, AR, EGF in addition to heregulin.
INCB3619 abrogates heregulin activation and heregulin-dependent HER3 signaling and increases gefitinib sensitivity in A549 cells.
INCB3619 induces apoptosis in A549 cells and has antitumor activity in the A549 xenograft model.
