NVP-BGT226
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BGT226 (NVP-BGT226) 是PI3K/mTOR的新型选择性抑制剂，其对PI3Kα、PI3Kβ和PI3Kγ的IC50值分别为4 nM、63 nM和38 nM [1]。
磷脂酰肌醇-3-激酶（PI3K）通路是胰腺癌最常见的活化信号通路之一，是新治疗策略的潜在靶点。
NVP-BGT226是PI3K/雷帕霉素哺乳动物靶点（mTOR）的新型双重抑制剂。相比于未处理的对照组，NVP-BGT226处理24-72小时后以浓度而非时间依赖的方式使细胞活力下降到约50% [1]。双重PI3K/mTOR抑制剂NVP-BGT226诱导G0/G1停滞，部分通过Survivin的下调起作用。NVP-BGT226高效抑制多种细胞系的生长活性，包括SCC4、TU183和KB细胞系，IC50值的范围从7.4到30.1 nM [2]。
在FaDu细胞异体移植小鼠模型中，BGT226以剂量依赖的方式抑制肿瘤生长。按2.5和5 mg/kg的剂量口服BGT226 3周造成第21天肿瘤生长分别降低34.7%和76.1%（相比于对照组）。BGT226具有与雷帕霉素相当的肿瘤生长抑制作用。两组的最终肿瘤体积都比LY294002处理或对照组显著减小[2]。
参考文献：
[1]. 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. TUMOR BIOLOGY, 2014, 33(3): 757-765.
[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): 7116-7126.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 650.6 |
| Cas No. | 1245537-68-1 |
| Formula | C28H25F3N6O2·C4H4O4 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥16.28 mg/mL in DMSO with gentle warming |
| Chemical Name | (Z)-but-2-enedioic acid;8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one |
| SDF | Download SDF |
| Canonical SMILES | CN1C2=CN=C3C=CC(=CC3=C2N(C1=O)C4=CC(=C(C=C4)N5CCNCC5)C(F)(F)F)C6=CN=C(C=C6)OC.C(=CC(=O)O)C(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | BGT226 (NVP-BGT226) 是1类PI3K/mTOR的新型选择性抑制剂，其对PI3Kα、PI3Kβ和PI3Kγ的IC50值分别为4 nM、63 nM和38 nM。 | |||||
| 靶点 | PI3Kα | PI3Kγ | PI3Kβ | |||
| IC50 | 4 nM | 38 nM | 63 nM | |||
质量控制和MSDS
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化学结构
