BGT226(Synonyms: NVP-BGT226)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BGT226 (Synonyms: NVP-BGT226)

BGT226 (NVP-BGT226) 是一种 PI3K (针对 PI3Kα，PI3Kβ，PI3Kγ 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。

BGT226(Synonyms: NVP-BGT226)

BGT226 Chemical Structure

CAS No. : 915020-55-2

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BGT226 的其他形式现货产品:

BGT226 maleate

生物活性

BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/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

 

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

534.53

Formula

C28H25F3N6O2
CAS 号

915020-55-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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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