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NVP-BGT226

Chemical Structure : NVP-BGT226

CAS No.: 1245537-68-1

NVP-BGT226 (BGT226;NVP-BGT 226;BGT-226)

Catalog No.: PC-43503Not For Human Use, Lab Use Only.

NVP-BGT226 (BGT226) is a potent, dual PI3K/mTOR inhibitor with a preference for PI3Kα (wild type and mutated) and mTOR ( PI3Kα, PI3Kβ and PI3Kγ, IC50=4, 63 and 38 nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NVP-BGT226 (BGT226) is a potent, dual PI3K/mTOR inhibitor with a preference for PI3Kα (wild type and mutated) and mTOR ( PI3Kα, PI3Kβ and PI3Kγ, IC50=4, 63 and 38 nM).
NVP-BGT226 displays potent antiproliferative activity against various human head and neck cancer cell lines in vitro (IC50=7.4-30.1 nM).
NVP-BGT226 downregulates the expression levels of the downstream proteins p-p70S6K and p-4E-BP1 in cells, induces cell-cycle arrest at the G0-G1 phase at 60 nM.
NVP-BGT226 significantly delays tumor growth in a dose-dependent manner, along with suppressed cytoplasmic expression of p-p70S6K and the presence of autophagosome formation in xenografted animal modes.

Physicochemical Properties

M.Wt 650.60
Formula C32H29F3N6O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one with maleic acid

References

1. Baumann P, et al. Anticancer Drugs. 2012 Jan;23(1):131-8.

2. Chang KY, et al. Clin Cancer Res. 2011 Nov 15;17(22):7116-26.

3. Sanchez CG, et al. Breast Cancer Res. 2011 Mar 1;13(2):R21.

4. Glienke W, et al. Tumour Biol. 2012 Jun;33(3):757-65.

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