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  1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    mTOR
    Autophagy

BGT226 (Synonyms: NVP-BGT226)

目录号: HY-13334A
Data Sheet产品使用指南

BGT226 (NVP-BGT226) 是一种 PI3K(针对PI3KαPI3KβPI3Kγ的IC50分别是4 nM,63 nM,38 nM ) /mTOR 双抑制剂,对人头颈癌细胞具有较强的生长抑制活性。

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BGT226 Chemical Structure

BGT226 Chemical Structure

CAS No. : 915020-55-2

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BGT226 的其他形式现货产品:

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的科研文献

  • Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.
  • Harvard Medical School LINCS LIBRARY

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  • 参考文献

Description

BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα,PI3KβandPI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells[1][2].

IC50 & Target[1]

PI3Kα

4 nM (IC50)

PI3Kβ

63 nM (IC50)

PI3Kγ

38 nM (IC50)

mTOR

 

Autophagy

 

In Vitro

BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively[2].
The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines[2].

Cell Viability Assay[2]

Cell Line:FaDu cells; OECM1 cells
Concentration:10, 100, 1000, 10000 nM
Incubation Time:
Result:Inhibited FaDu and OECM1 cells growth with IC50s of 23.1±7.4 and 12.5±5.1 nM, respectively.

Western Blot Analysis[2]

Cell Line:FaDu cells; OECM1 cells
Concentration:200 nM
Incubation Time:24 hours
Result:p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased.
In Vivo

BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control[2].

Animal Model:Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model[2]
Dosage:2.5 and 5 mg/kg
Administration:Oral administration; 21 days
Result:Caused 34.7% and 76.1% reduction of the tumor growth.
References
  • [1].Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408.

    [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 Nov 15;17(22):7116-26.

Molecular Weight

534.53

Formula

C₂₈H₂₅F₃N₆O₂

CAS No.

915020-55-2

SMILES

O=C(N1C2=CC=C(N3CCNCC3)C(C(F)(F)F)=C2)N(C)C4=C1C5=CC(C6=CC=C(OC)N=C6)=CC=C5N=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Data Sheet (109 KB)产品使用指南 (1213 KB)
  • [1].Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408.

    [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 Nov 15;17(22):7116-26.

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产品名称:
BGT226
目录号:
HY-13334A
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BGT226

Cat. No.: HY-13334A