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Cat. No. Name Size Price Add Cart
KI0641NVP-BGT2265 mg$432
NVP-BGT22610 mg$630
NVP-BGT22650 mg$1760
NVP-BGT226200 mg$4200

Chemical Characteristic

Product NameNVP-BGT226
SynonymsBGT226
CAS No.1245537-68-1
Molecular Weight 650.6
FormulaC28H25F3N6O2.C4H4O4
Chemical Structure

Biological activities

NVP-BGT226 is a dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) (both mTORC1 and mTORC2) inhibitor. NVP-BGT226 effectively inhibits phosphorylation of Akt, mTOR and S6 target proteins and reduces clonogenic survival in irradiated tumor cells. NVP-BGT226 inhibits phosphorylation of Ser473 Akt, Ser2448 mTOR, and Ser240/244 S6 in SQ20B cells at concentration of 5 nM. NVP-BGT226 enhances persistence of residual γH2AX foci after irradiation.[1] NVP-BGT226 induces predominantly G0/G1 cell cycle arrest. [2] NVP-BGT226 induces cancer cell death through an apoptosis-independent pathway. NVP-BGT226 induces autophagy as indicated by the aggregation and up-regulation of the microtubule-associated protein light chain 3B-II, and p62 degradation. NVP-BGT226 displays potent growth inhibitory activity against all tested cell lines (nine HNSCC cell lines and one NPC cell line), with IC50 ranging from 7.4 to 30.1 nM. NVP-BGT226 increases FaDu cells in G0/G1 phase at the concentration of 60 nM, and reaches the plateau at the concentration of 120 nM. In xenografted animal model, NVP-BGT226 significantly delays tumor growth in a dose-dependent manner, along with suppressed cytoplasmic expression of p-p70 S6 kinase and the presence of autophagosome formation. [3]

Protocols

NVP-BGT226 is dissolved in DMSO as 10 mM stock solution and kept frozen (-20°C) until use. [2]

References

[1] Fokas E, et al. NVP-BEZ235 and NVP-BGT226, dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitors, enhance tumor and endothelial cell radiosensitivity. Radiat Oncol. 2012, 7: 48. 閵嗏偓閵嗏偓
[2] Glienke W, et al. The dual PI3K/mTOR inhibitor NVP-BGT226 induces cell cycle arrest and regulates Survivin gene expression in human pancreatic cancer cell lines. Tumour Biol. 2012, 33(3): 757-765. 閵嗏偓閵嗏偓
[3] 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. Clin Cancer Res. 2011, 17(22): 7116-7126. 閵嗏偓閵嗏偓

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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