| Molecular Weight: | 534.53 |
| Formula: | C28H25F3N6O2 |
| Purity: | ≥98% |
| CAS#: | 1245537-68-1 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | 8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(3-(trifluoromethyl)piperazin-1-yl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with an IC50
~1 nM. In cellular assays it could produce nearly complete inhibition
of PI3K signaling at low nanomolar (<50 3="" 7="" nm)="" concentrations.="" flow="" cytometric="" analysis="" revealed="" an="" accumulation="" of="" cells="" in="" the="" g0–g1="" phase="" with="" a="" concomitant="" loss="" s-phase.="" tunel="" assay="" and="" caspase="" parp="" indicated="" that="" bgt226="" induced="" cancer="" cell="" death="" through="" apoptosis="" independent="" pathway.="" autophagy="" as="" by="" aggregation="" upregulation="" microtubule-associated="" protein="" light="" chain="" 3b-ii,="" p62="" degradation.="" it="" is="" i="" ii="" clinical="" trials="" for="" treatment="" advanced="" solid="" tumors.<="" span="">
How to Use:
- In vitro: BGT226 was used at 0.2 µM concentration in cellular assays to investigate its effects on the PI3K/AKT signaling pathways.
- In vivo: BGT226 was dissolved in 90% NMP/10% PEG300 and orally dosed at 5mg/Kg once a day.
Reference:
- 1. 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. (2011) Clin Cancer Res. 17(22):7116-26.
- 2. Baumann P, et al. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. (2012) Anticancer Drugs. 23(1):131-8.
- 3. Sanchez CG, et al. Preclinical modeling of combined phosphatidylinositol-3-kinase inhibition with endocrine therapy for estrogen receptor-positive breast cancer. (2011) Breast Cancer Res. 13(2):R21
- 4. Fokas E, et al. NVP-BEZ235 and NVP-BGT226, dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitors, enhance tumor and endothelial cell radiosensitivity. (2012) Radiat Oncol. 7:48
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Products are for research use only. Not for human use. |
