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NVP-BGT226, PI3K/mTOR Dual Inhibitor

NVP-BGT226, PI3K/mTOR Dual Inhibitor

$89.00
A PI3K/mTOR dual inhibitor in clinical trials for advanced solid tumors.
Catalog No. Unit Price Qty
M66050-2s 2mg solid $89.00
M66050-2 10 mM in DMSO (0.375 mL) $89.00
M66050-50s 50mg solid $1050.00

Details

Product Information
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 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. 

 

Reference:

  1. 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. 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. 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. 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


Products are for research use only. Not for human use.

Description

Details

Product Information
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 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. 

 

Reference:

  1. 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. 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. 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. 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


Products are for research use only. Not for human use.

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