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NVP-BGT226 Sale

(Synonyms: NVP-BGT226 maleate) 目录号 : GC16145

A dual PI3K and mTOR inhibitor

NVP-BGT226 Chemical Structure

Cas No.:1245537-68-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,743.00
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5mg
¥1,187.00
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10mg
¥1,890.00
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50mg
¥5,712.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

BGT226 (NVP-BGT226) is a novel inhibitor of PI3K/mTOR for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. [1]
The phosphatidylinositol-3-kinase (PI3K) pathway is one of the most commonly activated signaling pathways in pancreatic cancer and is a target of interest for new therapeutic approaches.
NVP-BGT226 is a novel dual class PI3K/mammalian target of rapamycin (mTOR) inhibitor. When used NVP-BGT226, cell viability decreased within 24-72 h after exposure to about 50% compared to untreated control cells in a concentration- but not time-dependent manner. [1] The dual PI3K/mTOR inhibitor NVP-BGT226 induces G0/G1 arrest and acts partially via downregulation of Survivin. NVP-BGT226 potently inhibited growth activity of cell lines, including SCC4, TU183 and KB cell lines with the IC50 ranging from 7.4 to 30.1 nM. [2]
In a FaDu cell xenografted mouse model, BGT226 inhibited tumor growth in a dose-dependent manner in a FaDu cell xenografted mouse model. Oral administration of BGT226 at 2.5 and 5 mg/kg for 3 weeks caused 34.7% and 76.1% reduction of the tumor growth on day 21, respectively (compared with control). BGT226 displayed comparable inhibition against tumor growth to rapamycin. The final volume of both groups was significantly smaller than those treated with LY294002 or the control. [2]
References:
[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.

Chemical Properties

Cas No. 1245537-68-1 SDF
别名 NVP-BGT226 maleate
化学名 (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
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
分子式 C28H25F3N6O2.C4H4O4 分子量 650.6
溶解度 ≥ 16.275mg/mL in DMSO with gentle warming 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.537 mL 7.6852 mL 15.3704 mL
5 mM 0.3074 mL 1.537 mL 3.0741 mL
10 mM 0.1537 mL 0.7685 mL 1.537 mL
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