BGT226 NVP-BGT226 MTOR Inhibitors cas 1245537-68-1

BGT226 (NVP-BGT226) is a novel class IPI3K/mTORinhibitor for PI3K// withIC50of 4 nM/63 nM/38 nM. Phase 1/2.

NVP-BGT226 (BGT226) specifically inhibits p110, p110, p110, and p110, with a preference for the -isoform (wild type and mutated), and mTOR, with no significant inhibitory activity against other tested kinases. The IC₅₀of NVP-BGT226 for the individual isoforms of the class I PI3Ks is (±standard deviation) PI3K 4 nM (±1), PI3K 63 nM (±10), and PI3K 38 nM (±23) as determined by filter-binding assay. In preclinical studies, NVP-BGT226 inhibits cancer cell proliferation with IC₅₀values in the low nanomolar range and inhibits solid tumor growth in various mouse xenograft models, including glioblastoma multiforme, breast, and prostate cancer. To evaluate the antiproliferative activity of NVP-BGT226 (BGT226) against head and neck cancer cells, 9 HNSCC cell lines from different sites of the oral cavity and 1 NPC cell line with its cisplatin-resistant variant are used. NVP-BGT226 displays potent growth-inhibitory activity against all tested cell lines, with the IC₅₀ranging from 7.4 to 30.1 nM. Notably, both Detroit 562 and HONE-1 cells, which expressPIK3CAmutation H1047R, are still sensitive to the growth-inhibitory effect of NVP-BGT226 treatment. In addition, the sensitivity to NVP-BGT226 between HONE-1 cells and its cis