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BGT226 (NVP-BGT226)

BGT226 (NVP-BGT226) 1245537-68-1
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Chemical Information
Product name:BGT226 (NVP-BGT226) Purity:98%min
CAS NO:1245537-68-1 Solubility:Soluble in DMSO
Molecular Formula:C32H29F3N6O6 Package:Packaging according to customer requirements
Molecular Weight:650.6 Storage:Store at -20℃
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Remarks

BGT226 (NVP-BGT226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.

NVP-BGT226 (BGT226) specifically inhibits p110α, p110β, p110δ, and p110γ, with a preference for the α-isoform (wild type and mutated), and mTOR, with no significant inhibitory activity against other tested kinases. The IC50 of NVP-BGT226 for the individual isoforms of the class I PI3Ks is (±standard deviation) PI3Kα 4 nM (±1), PI3Kβ 63 nM (±10), and PI3Kγ 38 nM (±23) as determined by filter-binding assay. In preclinical studies, NVP-BGT226 inhibits cancer cell proliferation with IC50 values in the low nanomolar range and inhibits solid tumor growth in various mouse xenograft models, including glioblastoma multiforme, breast, and prostate cancer[1]. 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 IC50 ranging from 7.4 to 30.1 nM. Notably, both Detroit 562 and HONE-1 cells, which express PIK3CA mutation 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 cisplatin-resistant variant is almost identical[2].

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