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BGT226 maleate

Cat. No. M1735
BGT226 maleate Structure
Synonym:

NVP-BGT226

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.

References

[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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