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Product Infomation
Product NameBGT226 maleate
CAS No.

1245537-68-1

Molecular Weight

650.60

Formula

C₃₂H₂₉F₃N₆O₆

SMILES

COC1=CC=C(C=N1)C2=CC=C(C3=C2)N=CC(N4C)=C3N(C4=O)C5=CC=C(C(C(F)(F)F)=C5)N6CCNCC6.OC(/C=C\C(O)=O)=O

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Product description

Description

BGT226 maleate (NVP-BGT226 maleate) 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].


IC50 & Target

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PI3Kα

4 nM (IC50)


In Vitro

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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].





Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

[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.