TAE684

TAE684 is a highly potent and selective **small molecule inhibitor** of receptor tyrosine kinases, primarily targeting **anaplastic lymphoma kinase (ALK)** and the **nucleophosmin-anaplastic lymphoma kinase (NPM-ALK) fusion kinase**[4][1][6]. It was originally developed as an experimental agent to inhibit ALK-driven signaling pathways in tumors, especially in ALK-positive anaplastic large cell lymphoma (ALCL) and cancer models with ALK rearrangements or mutations. TAE684 demonstrates nanomolar-range IC₅₀ for ALK in biochemical and cellular assays, causing cell cycle arrest and apoptosis specifically in ALK- or NPM-ALK-dependent cell lines, and induces significant tumor regression in xenograft models. Experimental data also show selectivity for ALK over other kinases, although some activity against Insulin receptor (InsR) and leucine-rich repeat kinase 2 (LRRK2) has been observed. TAE684 exhibits good oral bioavailability and favorable pharmacokinetic properties in animal models[1][6][4]. While showing strong preclinical efficacy, TAE684 has remained a research compound and is not approved for clinical use.

Other names

5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)pyrimidine-2,4-diamine761439-42-3