|Solubility:||DMSO up to 50 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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 nM) concentrations. Flow cytometric analysis revealed an accumulation of cells in the G0–G1 phase with a concomitant loss in the S-phase. TUNEL assay and the analysis of Caspase 3/7 and PARP indicated that BGT226 induced cancer cell death through an apoptosis independent pathway. BGT226 induced autophagy as indicated by the aggregation and upregulation of the microtubule-associated protein light chain 3B-II, and p62 degradation. It is in the phase I/II clinical trials for the treatment of advanced solid tumors.
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.
- 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.
- 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.
- 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
- 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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