BGT226 (NVP-BGT226) 是一种 PI3K (针对 PI3Kα，PI3Kβ，PI3Kγ 的 IC50分别是4 nM，63 nM，38 nM ) /mTOR 双抑制剂，对人头颈癌细胞具有较强的生长抑制活性。
CAS：915020-55-2
分子式：C28H25F3N6O2
分子量：534.53
纯度：98%
存储：Store at -20°C

Background:

BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells[1][2]. PI3Kα|4 nM (IC50)|PI3Kβ|63 nM (IC50)|PI3Kγ|38 nM (IC50)|mTOR Autophagy

BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively[2].The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines[2]. Cell Viability Assay[2] Cell Line: FaDu cells; OECM1 cells

BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control[2]. Animal Model: Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model[2]

[1]. Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408. [2]. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26.