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BGT226 maleate

Cat. No. M1735
BGT226 maleate Structure


Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 195  USD195 In stock
50mg USD 650  USD650 In stock
100mg USD 950  USD950 In stock
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Quality Control & Documentation
Biological Activity

BGT226 (NVP-BGT226) is a novel phosphoinositide 3-kinase/mTOR dual inhibitor. BGT226 (NVP-BGT226) displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.

Protocol (for reference only)
Cell Experiment
Cell lines FaDu, Detroit 562, HONE-1 and HONE-1-C15 cells line
Preparation method Growth-inhibition assay.
Cells in the logarithmic growth phase were cultured at a density of 5,000 to 20,000 cells per milliliter per well in a 24-well plate. The cells were exposed to various concentrations of BGT226 for 3 generation times. At the end of the incubation period, cells were fixed and stained with 50% ethanol containing 0.5% methylene blue for 30 minutes. The resulting colored residues were dissolved in 1% N-lauroyl-sarcosine, and optical density was read at 550 nm using a microplate reader. The IC50 value resulting from 50% inhibition of cell growth was calculated graphically as a comparison with control groups. Each point represents the average of at least 3 independent experiments run in duplicate.
Concentrations IC50 ranging from 7.4 to 30.1 nmol/L
Incubation time 48 h
Animal Experiment
Animal models human FaDu xenografted mice
Formulation dissolved in 90% N-methyl-2-pyrrolidone (NMP)/10% PEG300
Dosages 3.5 and 5mg/kg once a day for 21 consecutive days
Administration orally
Chemical Information
Molecular Weight 650.6
Formula C32H29F3N6O6
CAS Number 1245537-68-1
Form Solid
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Markman et al. Ann Oncol. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors.

[2] Glienke et al. Tumour Biol. The dual PI3K/mTOR inhibitor NVP-BGT226 induces cell cycle arrest and regulates Survivin gene expression in human pancreatic cancer cell lines.

[3] Chang KY, et al. Clin Cancer Res. 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.

[4] Baumann et al. Anticancer Drugs. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma.

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Keywords: BGT226 maleate, NVP-BGT226 supplier, PI3K, inhibitors, activators

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