INCB3619 (INCB-3619) is a novel, potent, orally bioavailable and highly specific ADAM10 inhibitor, but also markedly inhibits ADAM17, MMP12 and MMP15 with anticancer activity. INCB3619 inhibits the EGFR ligand signaling in the EGFR autocrine cell line NCI-H1666 and sensitizes it to gefitinib. In Min mice, INCB3619 reduced EGFR
signals in adenomas and inhibited intestinal tumor multiplicity
(P < 0.05). In the AOM model, colonocyte ADAM17 deletion
reduced EGFR signals and colonic tumor development (P < 0.05).
Finally, ADAM17 was upregulated >2.5-fold in human malignant
colonocytes.
纯度:≥98%
CAS:791826-72-7