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BGT226 maleate

产品编号 T6072 CAS 1245537-68-1

别名: BGT226, NVP-BGT226 (maleate), NVP-BGT226

BGT226 maleate (NVP-BGT226) 是一种 PI3K/mTOR 双抑制剂，针对 PI3Kα、PI3Kβ、PI3Kγ的 IC50分别是4 nM、63 nM、38 nM，对人头颈癌细胞具有较强的生长抑制活性。

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BGT226 maleate, CAS 1245537-68-1

规格	价格/CNY	货期
1 mg	￥ 413	现货
5 mg	￥ 997	现货
10 mg	￥ 1,620	现货
25 mg	￥ 3,320	现货
50 mg	￥ 5,390	现货
100 mg	￥ 7,390	现货
500 mg	￥ 14,800	现货
1 mL * 10 mM (in DMSO)	￥ 1,420	现货

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其他形式的 BGT226 maleate:

BGT226
现货

选择批次

纯度: 98.78%

纯度: 97.75%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	BGT226 maleate (NVP-BGT226) is a class I PI3K/mTOR inhibitor for PI3Kα/β/γ (IC50: 4/63/38 nM) .
靶点活性	PI3Kγ:38 nM, PI3Kα:4 nM, PI3Kβ:63 nM
体外活性	The anti-proliferative and pro-apoptotic effects of NVP-BGT226 are independent of bcr-abl status. The activation of the AKT/mTOR signal cascade is suppressed by NVP-BGT226 in a concentration- and time-dependent manner. Flow cytometric analysis exhibits an accumulation of cells in the G(0)-G(1) phase with concomitant loss in the S-phase. NVP-BGT226 displays potent growth-inhibitory activity against all tested cell lines including SCC4, TU183 and KB cell lines with the IC50 ranging from 7.4 to 30.1 nM. Notably, both Detroit 562 and HONE-1 cells, which express PIK3CA mutation H1047R, are still sensitive to the growth-inhibitory effect of NVP-BGT226 treatment. In addition, the sensitivity to NVP-BGT226 between HONE-1 cells and its cisplatin-resistant variant is almost identical. Results of the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay and the analysis of caspase 3/7 and PARP indicates that NVP-BGT226 induces cancer cell death through an apoptosis-independent pathway. NVP-BGT226 induces autophagy as indicated by the aggregation and upregulation of the microtubule-associated protein light chain 3B-II, and p62 degradation. Gene silencing of Beclin1 or cotreatment of the autophagosome inhibitor, 3-methyladenine, inhibits the NVP-BGT226-induced autophagy and leads to the retrieval of colony survival.[2] NVP-BGT226 inhibits growth in common myeloma cell lines and primary myeloma cells (such as NCI-H929, U266, RPMI-8226 and OPM2 MM cell lines) at nanomolar concentrations in a time-dependent and dose-dependent manner. NVP-BGT226 inhibits phosphorylation of protein kinase B (Akt), P70S6k and 4E-BP-1 in a time-dependent and dose-dependent manner.
体内活性	In a xenografted animal model, NVP-BGT226 significantly delays tumor growth in a dose-dependent manner, along with suppressed cytoplasmic expression of p-p70 S6 kinase and the presence of autophagosome formation. NVP-BGT226 inhibits tumor growth in a dose-dependent manner in a FaDu cell xenografted mouse model. Oral administration of NVP-BGT226 at 2.5 and 5 mg/kg for 3 weeks causes 34.7% and 76.1% reduction of the tumor growth on day 21, respectively (compared with control). NVP-BGT226 displays comparable inhibition against tumor growth to rapamycin. The final volume of both groups is significantly smaller than those treated with LY294002 (a PI3K inhibitor) or the control. [2]
细胞实验	NCI-H929, U266, RPMI-8226 and OPM2 MM cells are seeded in 96-well plates at a concentration of 1.5 × 104 cells/well in RPMI medium supplemented with 10% fetal bovine serum with or without NVP-BGT226 that is to be tested. After 36 hours, BrdU-labelling solution is added (final concentration: 10 μM), and cells are cultured for another 12 hours in a humidified atmosphere (37 °C/5% CO2). Then, the plates are centrifuged (10 min, 300 g), and the supernatants are discarded. The plates are dried at 60 °C for 2 hours. After fixation with ethanol/HCl for 30 min at -20 °C, the DNA is partially digested by nuclease treatment for 30 min at 37 °C. The cells are washed three times with medium and incubated with anti-BrdU-POD labelling solution for 30 min at 37 °C. The anti-POD solution is removed and the cells are washed three times with washing buffer. The ABTS substrate solution is added, and absorbance is measured in a microplate reader at 405 nm with a reference wave length of 490 nm.(Only for Reference)

别名	BGT226, NVP-BGT226 (maleate), NVP-BGT226
分子量	650.6
分子式	C28H25F3N6O2·C4H4O4
CAS No.	1245537-68-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 28 mg/mL (43 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.537 mL	7.6852 mL	15.3704 mL	38.4261 mL
	5 mM	0.3074 mL	1.537 mL	3.0741 mL	7.6852 mL
	10 mM	0.1537 mL	0.7685 mL	1.537 mL	3.8426 mL
	20 mM	0.0769 mL	0.3843 mL	0.7685 mL	1.9213 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Markman B, et al. Ann Oncol, 2012, 23(9), 2399-2408. 2. Chang KY, et al. Clin Cancer Res, 2011, 17(22), 7116-7126. 3. Baumann P, et al. Anticancer Drugs, 2012, 23(1), 131-138. 4. Glienke W, et al. Tumour Biol, 2012, 33(3), 757-765.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BGT226 maleate 1245537-68-1 Apoptosis Autophagy PI3K/Akt/mTOR signaling PI3K mTOR BGT-226 NVP-BGT-226 BGT226 Mammalian target of Rapamycin Phosphoinositide 3-kinase inhibit BGT 226 Maleate NVP-BGT226 (maleate) NVP-BGT 226 BGT 226 NVP-BGT226 BGT226 Maleate BGT-226 maleate Inhibitor BGT-226 Maleate inhibitor

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BGT226 maleate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords