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NVP-BGT226 | PI3K/mTOR inhibitor

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Price:
$159.00
Catalog #:
C2482-2s
Quantity:


Product Description

NVP-BGT226 is a novel orally bioavailable dual PI3K/mTOR inhibitor. It selectively inhibits PI3K and both mTOR complexes mTORC1 and mTORC2, resulting in nearly complete phosphorylation-inhibition of P70S6 and 4E-BP1.

BGT226 demonstrated excellent cellular activities in inhibiting proliferations (IC50: 7-30 nM) of many tested cell lines. Notably, cells that express PIK3CA mutation H1047R are still sensitive to the growth-inhibition of BGT226. Flow cytometric analysis shows accumulation of cells in the G0-G1 phase with concomitant loss in the S-phase. BGT226 induces apoptosis or autophagy of some cancer cells at IC50 less than 25nM. In animal models, BGT226 significantly delays/inhibits tumor growth in a dose-dependent manner. BGT-226 represents a potential candidate for cancer therapy. It has entered phaseI/II clinical trials for treatment of advanced solid tumors (including breast cancer) [1-4].


Technical information:

Chemical Formula:   C28H25F3N6O2.C4H4O4
CAS #:   1245537-68-1
Molecular Weight:   650.6
Purity:   >98%
Appearance:   White
Chemical Name:   8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one Maleic acid
Solubility:   Up to 22 mM in DMSO
Synonyms:   NVP-BGT226, BGT226

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Badura S, et al. Poster Abstracts. Differential Suppressive Effects of Selective PI3K and mTOR and Dual PI3K/mTORC1/C2 Inhibition on Long-Term Cultured Primary Human Acute Lymphoblastic Leukemia (ALL) Cells Implicate a Distinct Role of mTORC2 https://ash.confex.com/ash/2010/webprogram/Paper33127.html
2. 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):7116-26. Pubmed ID: 21976531
3. Baumann P, et al. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012. 23(1):131-8. Pubmed ID: 21959532
4. http://clinicaltrials.gov/ct2/show/NCT00600275

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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cancer  mTOR  PI3K  
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